PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 9681140-3 1998 Incorporation of piperazine into the 4,5-dihydro-1H-benzo[g]indazoles in place of piperidine gave a novel series of high affinity, selective, orally bioavailable hD4 ligands, such as 16, with improved selectivity over ion channels. Piperazine 17-27 Rho GDP dissociation inhibitor beta Homo sapiens 162-165 9582295-15 1998 Addition of SIN-1 or authentic peroxynitrite to solutions of Good"s buffers resulted in the formation of piperazine-derived radical cations as detected by ESR spectroscopy. Piperazine 105-115 MAPK associated protein 1 Homo sapiens 12-17 8941383-2 1996 The substitution of the piperazine ring in the GBR structure with other diamine moieties resulted in the retention of the high affinity of new ligands for the DAT. Piperazine 24-34 solute carrier family 6 member 3 Homo sapiens 159-162 9436302-4 1997 The activities of several phenylpiperazines, in combination with their crystal structures and conformational characteristics, lead to the hypothesis that the conformation for which the piperazine ring and the phenyl ring are approximately co-planar should be the 5-HT2C receptor "activating" conformation. Piperazine 32-42 5-hydroxytryptamine receptor 2C Homo sapiens 263-269 9238639-0 1996 Rationally designed non-peptides: variously substituted piperazine libraries for the discovery of bradykinin antagonists and other G-protein-coupled receptor ligands. Piperazine 56-66 kininogen 1 Homo sapiens 98-108 8905919-4 1996 The proton nmr longitudinal relaxation rate study indicated that the paramagnetic effects of the haem iron of CYP1A2 were observed in protons of enoxacin with a 1,8-naphthyridine skeleton and its 4"-nitrogen atom on the 7-piperazine ring probably participated in specific binding to the haem iron. Piperazine 220-232 cytochrome P450, family 1, subfamily a, polypeptide 2 Rattus norvegicus 110-116 8848002-6 1995 A region including transmembrane domains 1-3 of the norepinephrine transporter also contributes to the interaction of desipramine and nisoxetine, whereas the analogous region of the dopamine transporter influences the affinity for piperazine derivatives (e.g., GBR12909 and LR1111) that are selective for the dopamine transporter. Piperazine 231-241 solute carrier family 6 member 3 Homo sapiens 182-202 7482633-3 1995 Delta 5.7-Sterol delta 7-reductase was inhibited by both RPR 101821, a protonated cyclohexylamine, and BM 15.766, a piperazine derivative, with IC50 values of 1 microM. Piperazine 116-126 7-dehydrocholesterol reductase Homo sapiens 10-34 8302284-1 1994 P-type Ca2+ channels in cerebellar Purkinje neurons and N-type Ca2+ channels in sympathetic neurons were found to be inhibited by D2 dopamine receptor antagonists with diverse structures, including phenothiazines (chlorpromazine and thioridazine), diphenylbutylpiperidines (fluspirilene and pimozide), butyrophenones (haloperidol and spiperone), and a piperazine (fluphenazine). Piperazine 352-362 dopamine receptor D2 Homo sapiens 130-150 7741042-1 1994 CGP 47969A is a novel piperazine derivative that inhibits the synthesis of inflammatory cytokines, such as interleukin-1 alpha (IL-1), IL-1 beta and tumor necrosis factor alpha (TNF), in human monocytes stimulated with lipopolysaccharide (LPS), zymosan or IL-1 itself. Piperazine 22-32 interleukin 1 alpha Homo sapiens 107-126 7741042-1 1994 CGP 47969A is a novel piperazine derivative that inhibits the synthesis of inflammatory cytokines, such as interleukin-1 alpha (IL-1), IL-1 beta and tumor necrosis factor alpha (TNF), in human monocytes stimulated with lipopolysaccharide (LPS), zymosan or IL-1 itself. Piperazine 22-32 interleukin 1 beta Homo sapiens 128-132 7741042-1 1994 CGP 47969A is a novel piperazine derivative that inhibits the synthesis of inflammatory cytokines, such as interleukin-1 alpha (IL-1), IL-1 beta and tumor necrosis factor alpha (TNF), in human monocytes stimulated with lipopolysaccharide (LPS), zymosan or IL-1 itself. Piperazine 22-32 interleukin 1 beta Homo sapiens 135-144 7741042-1 1994 CGP 47969A is a novel piperazine derivative that inhibits the synthesis of inflammatory cytokines, such as interleukin-1 alpha (IL-1), IL-1 beta and tumor necrosis factor alpha (TNF), in human monocytes stimulated with lipopolysaccharide (LPS), zymosan or IL-1 itself. Piperazine 22-32 tumor necrosis factor Homo sapiens 149-176 7741042-1 1994 CGP 47969A is a novel piperazine derivative that inhibits the synthesis of inflammatory cytokines, such as interleukin-1 alpha (IL-1), IL-1 beta and tumor necrosis factor alpha (TNF), in human monocytes stimulated with lipopolysaccharide (LPS), zymosan or IL-1 itself. Piperazine 22-32 tumor necrosis factor Homo sapiens 178-181 7741042-1 1994 CGP 47969A is a novel piperazine derivative that inhibits the synthesis of inflammatory cytokines, such as interleukin-1 alpha (IL-1), IL-1 beta and tumor necrosis factor alpha (TNF), in human monocytes stimulated with lipopolysaccharide (LPS), zymosan or IL-1 itself. Piperazine 22-32 interleukin 1 beta Homo sapiens 135-139 34364049-3 2021 In this work, three series of new piperazine urea TRPV1 antagonists were designed, synthesized and evaluated based on classical TRPV1 antagonists BCTC and GRT12360. Piperazine 34-44 transient receptor potential cation channel subfamily V member 1 Homo sapiens 50-55 8383921-18 1993 Piperazine ring-cleaved compounds and naphthyridine nuclei were shown to be most active inhibitors of cytochrome P-4501A2. Piperazine 0-10 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 102-121 1331748-9 1992 Using [3H]5-HT as the basis for a radioligand binding assay, the relative affinities of several tryptamine and piperazine derivatives for the cloned 5-HT2F receptor correlated with their relative potencies to contract the rat stomach fundus. Piperazine 111-121 5-hydroxytryptamine receptor 2B Rattus norvegicus 149-155 1351684-4 1992 Most notably, metergoline and serotonergic piperazine derivatives, as a group, display 3- to 8-fold lower affinity for the 5HT1D beta receptor than for the 5HT1D receptor, whereas both receptors display similar affinities for tryptamine derivatives, including the antimigraine drug sumatriptan. Piperazine 43-53 5-hydroxytryptamine receptor 1B Homo sapiens 123-133 1351684-4 1992 Most notably, metergoline and serotonergic piperazine derivatives, as a group, display 3- to 8-fold lower affinity for the 5HT1D beta receptor than for the 5HT1D receptor, whereas both receptors display similar affinities for tryptamine derivatives, including the antimigraine drug sumatriptan. Piperazine 43-53 5-hydroxytryptamine receptor 1D Homo sapiens 123-128 2288479-2 1990 Using piperazine, imidazolidine and 1,2-diaminocyclohexane, resp., isoxazoles with partially rigid chains at C-5 are formed. Piperazine 6-16 complement C5 Rattus norvegicus 109-112 2323200-0 1990 Contact dermatitis due to piperazine in a plastic watch strap. Piperazine 26-36 serine/threonine kinase receptor associated protein Homo sapiens 56-61 34571173-0 2021 Piperazine squaric acid diamides, a novel class of allosteric P2X7 receptor antagonists. Piperazine 0-10 purinergic receptor P2X 7 Homo sapiens 62-75 34571173-3 2021 Herein we describe the development of novel P2X7R antagonists, incorporating piperazine squaric diamides as a central element. Piperazine 77-87 purinergic receptor P2X 7 Homo sapiens 44-49 33349069-0 2021 Novel piperazine-chalcone hybrids and related pyrazoline analogues targeting VEGFR-2 kinase; design, synthesis, molecular docking studies, and anticancer evaluation. Piperazine 6-16 kinase insert domain receptor Homo sapiens 77-84 33349069-1 2021 New piperazine-chalcone hybrids and related pyrazoline derivatives have been designed and synthesised as potential vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitors. Piperazine 4-14 kinase insert domain receptor Homo sapiens 115-160 33349069-1 2021 New piperazine-chalcone hybrids and related pyrazoline derivatives have been designed and synthesised as potential vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitors. Piperazine 4-14 kinase insert domain receptor Homo sapiens 162-169 34990933-4 2022 Both series yielded low micromolar selective inhibitors of human MAO-B, namely indole 2 (IC50 = 12.63 +- 1.21 microM) and piperazine 39 (IC50 = 19.25 +- 4.89 microM), which is comparable to selective MAO-B inhibitor isatin (IC50 = 6.10 +- 2.81 microM), yet less potent in comparison to safinamide (IC50 = 0.029 +- 0.002 microM). Piperazine 122-132 monoamine oxidase B Homo sapiens 65-70 34714059-2 2021 Herein, an integration of multirole regulations was synchronously realized using poly(acrylic acid) (PAA) as an active additive in a piperazine (PIP) aqueous phase. Piperazine 133-143 prolactin induced protein Homo sapiens 145-148 34795851-0 2021 Novel Substituted Piperazine Amide Compounds as Indoleamine-2,3-dioxygenase (IDO) Inhibitors. Piperazine 18-28 indoleamine 2,3-dioxygenase 1 Homo sapiens 48-75 34795851-0 2021 Novel Substituted Piperazine Amide Compounds as Indoleamine-2,3-dioxygenase (IDO) Inhibitors. Piperazine 18-28 indoleamine 2,3-dioxygenase 1 Homo sapiens 77-80 34674410-0 2022 Novel thiazolyl-hydrazone derivatives including piperazine ring: synthesis, in vitro evaluation, and molecular docking as selective MAO-A inhibitor. Piperazine 48-58 monoamine oxidase A Homo sapiens 132-137 34676043-1 2021 This work surveys a variety of diamino-heterocycles as an isosteric replacement for the piperazine substructure of our previously disclosed piperarinyl-tetrahydroisoquinoline containing CXCR4 antagonists. Piperazine 88-98 chemokine (C-X-C motif) receptor 4 Mus musculus 186-191 34333397-0 2021 Adenosine deaminase - A target for new piperazine derivatives. Piperazine 39-49 adenosine deaminase Bos taurus 0-19 34333397-4 2021 This work describes the inhibition of bovine ADA by new synthesized piperazine compounds. Piperazine 68-78 adenosine deaminase Bos taurus 45-48 34333423-0 2021 Pentacyclic triterpene carboxylic acids derivatives integrated piperazine-amino acid complexes for alpha-glucosidase inhibition in vitro. Piperazine 63-73 sucrase-isomaltase Homo sapiens 99-116 35264969-9 2022 The presence of a halogen substitute, regardless of the position, in the fluorophenyl moiety next to the piperazine ring was essential for the inhibitory effects on ENT1 and ENT2. Piperazine 105-115 solute carrier family 29 member 1 (Augustine blood group) Homo sapiens 165-169 35611784-0 2022 Molecular Modelling and Virtual Screening to Identify New Piperazine Derivatives as Potent Human 5-HT1A Antagonists and Reuptake Inhibitors. Piperazine 58-68 5-hydroxytryptamine receptor 1A Homo sapiens 97-103 34118788-6 2021 Among the three synthesized agents, the piperazine substituted BG-P400-PAT exhibited potent integrin alphavbeta3 antagonism and reduced neuroblastoma tumor growth and cancer cell viability by >90%. Piperazine 40-50 integrin subunit alpha V Homo sapiens 92-112 35264969-9 2022 The presence of a halogen substitute, regardless of the position, in the fluorophenyl moiety next to the piperazine ring was essential for the inhibitory effects on ENT1 and ENT2. Piperazine 105-115 solute carrier family 29 member 2 Homo sapiens 174-178 35075146-3 2022 Our ITC results show that these inhibitors have similar binding affinity with both GDP-bound and GTP-bound KRAS(G12D), and our crystallographic studies reveal the structural basis of inhibitor binding-induced switch-II pocket in KRAS(G12D), experimentally confirming the formation of a salt bridge between the piperazine moiety of the inhibitors and the Asp12 residue of the mutant protein. Piperazine 310-320 KRAS proto-oncogene, GTPase Homo sapiens 107-111 35075146-3 2022 Our ITC results show that these inhibitors have similar binding affinity with both GDP-bound and GTP-bound KRAS(G12D), and our crystallographic studies reveal the structural basis of inhibitor binding-induced switch-II pocket in KRAS(G12D), experimentally confirming the formation of a salt bridge between the piperazine moiety of the inhibitors and the Asp12 residue of the mutant protein. Piperazine 310-320 KRAS proto-oncogene, GTPase Homo sapiens 229-233 6130141-7 1982 The observed ratio of Ka1/Ka2 in I-III, 2.75 X 10(5)-7.76 X 10(5), was attributed to solven- and space-mediated field effects and electrostatic induction between nitrogen atoms in the piperazine ring. Piperazine 184-194 glutamate ionotropic receptor kainate type subunit 4 Homo sapiens 22-29 35059126-1 2022 We recently disclosed a set of heteroaryl-fused piperazine inhibitors of BACE1 that combined nanomolar potency with good intrinsic permeability and low Pgp-mediated efflux. Piperazine 48-58 beta-secretase 1 Homo sapiens 73-78 35059126-1 2022 We recently disclosed a set of heteroaryl-fused piperazine inhibitors of BACE1 that combined nanomolar potency with good intrinsic permeability and low Pgp-mediated efflux. Piperazine 48-58 phosphoglycolate phosphatase Homo sapiens 152-155 3372356-3 1988 Structure-cytotoxicity relationships studies have indicated that the C-3 and C-6 disubstituted piperazine-2,5-diones are structurally required for significant cytotoxicity, and the neihumicin-like C-3 and C-6 disubstituted unsymmetrical piperazine derivatives are, in general, more cytotoxic than the corresponding symmetrical piperazine-2,5-diones. Piperazine 95-105 complement C3 Homo sapiens 69-72 2907712-1 1988 One piperazine derivative of tetraline (with code P11), possessing hypotensive and anti-hypertensive activity, is studied. Piperazine 4-14 S100 calcium binding protein A10 Rattus norvegicus 50-53 3224653-3 1988 The piperazine derivative flunarizine, however, which is known to suppress epileptic discharges in hippocampal CA3 neurons (Bingmann and Speckmann 1986), showed no significant antiepileptic effects in the explanted neocortical neurons. Piperazine 4-14 carbonic anhydrase 3 Rattus norvegicus 111-114 2886925-0 1987 Piperazine derivatives including the putative anxiolytic drugs, buspirone and ipsapirone, are agonists at 5-HT1A receptors negatively coupled with adenylate cyclase in hippocampal neurons. Piperazine 0-10 5-hydroxytryptamine (serotonin) receptor 1A Mus musculus 106-112 3744574-0 1986 Prevalence of specific IgE antibodies against piperazine in employees of a chemical plant. Piperazine 46-56 immunoglobulin heavy constant epsilon Homo sapiens 23-26 3744574-1 1986 In 5 out of 72 (7%) workers exposed to the asthma-inducing amine piperazine, specific IgE antibodies against a conjugate between human serum albumin and piperazine were demonstrated with RAST and RAST inhibition techniques. Piperazine 65-75 immunoglobulin heavy constant epsilon Homo sapiens 86-89 2997557-1 1985 The pharmacological action of a newly synthesized piperazine derivative of 2-aminotetralin (P11) on pre- and postsynaptic alpha-adrenoceptors of isolated rat vas deferens has been investigated. Piperazine 50-60 S100 calcium binding protein A10 Rattus norvegicus 92-95 2984944-4 1985 The dissociation constant of the interaction was 1.6 X 10(-7) M. Other proteins of high isoelectric points (lactoperoxidase, lysozyme, and particularly salmine sulfate) and a piperazine derivative inhibited hLf binding in a concentration-dependent manner. Piperazine 175-185 HLF transcription factor, PAR bZIP family member Homo sapiens 207-210 6849870-6 1983 The neighboring negative side chains in the peptide sequence also suggest that the single positive charge present on the piperazine nitrogens of trifluoperazine may interact with them and sterically block a region of interaction of calmodulin (CaM) and troponin C (TnC) with modulated proteins such as phosphodiesterase. Piperazine 121-131 tenascin Oryctolagus cuniculus 253-263 6849870-6 1983 The neighboring negative side chains in the peptide sequence also suggest that the single positive charge present on the piperazine nitrogens of trifluoperazine may interact with them and sterically block a region of interaction of calmodulin (CaM) and troponin C (TnC) with modulated proteins such as phosphodiesterase. Piperazine 121-131 tenascin Oryctolagus cuniculus 265-268 4827817-0 1974 Effect of castration on cholesterol metabolism and hepatic cytochrome P-450 in piperazine-treated male and female rabbits. Piperazine 79-89 cytochrome P-450 Oryctolagus cuniculus 59-75 33756235-4 2021 Among all the synthesised compounds, 9h with 4-(aminomethyl) piperidine linker and 14n with piperazine linker demonstrated good activity against human HDAC1 and HDAC6, respectively. Piperazine 92-102 histone deacetylase 1 Homo sapiens 151-156 34029971-0 2021 Amiridine-piperazine hybrids as cholinesterase inhibitors and potential multitarget agents for Alzheimer"s disease treatment. Piperazine 10-20 butyrylcholinesterase Homo sapiens 32-46 34029971-3 2021 Conjugates were moderate inhibitors of equine and human BChE with negligible fluctuation in anti-BChE activity, whereas anti-AChE activity was substantially dependent on N4-substitution of the piperazine ring. Piperazine 193-203 acetylcholinesterase (Cartwright blood group) Homo sapiens 125-129 33543794-3 2021 The combination of structural elements (heterocyclic nucleus, hydroxyalkyl chain, and 4-substituted piperazine), known to be critical for the affinity to 5-HT1A receptors, and the proper selection of substituents resulted in compounds with high specificity and affinity toward serotoninergic receptors. Piperazine 100-110 5-hydroxytryptamine receptor 1A Homo sapiens 154-160 33756235-4 2021 Among all the synthesised compounds, 9h with 4-(aminomethyl) piperidine linker and 14n with piperazine linker demonstrated good activity against human HDAC1 and HDAC6, respectively. Piperazine 92-102 histone deacetylase 6 Homo sapiens 161-166 33261900-4 2021 The replacement of piperazine in 3 with piperidine in compound 2, led to slightly reduced affinity towards the H3R (Ki = 3.17 and 7.70 nM, respectively). Piperazine 19-29 histamine receptor H3 Homo sapiens 111-114 33934107-4 2021 METHODS: A series of piperazine compounds that inhibited ALDH1A1 were identified and their inhibitory activity was characterized in vitro using purified recombinant enzymes and cell-based assay systems. Piperazine 21-31 aldehyde dehydrogenase family 1, subfamily A1 Mus musculus 57-64 33743158-0 2021 Piperazine-substituted chalcones: a new class of MAO-B, AChE, and BACE-1 inhibitors for the treatment of neurological disorders. Piperazine 0-10 monoamine oxidase B Homo sapiens 49-54 33743158-0 2021 Piperazine-substituted chalcones: a new class of MAO-B, AChE, and BACE-1 inhibitors for the treatment of neurological disorders. Piperazine 0-10 acetylcholinesterase (Cartwright blood group) Homo sapiens 56-60 33743158-0 2021 Piperazine-substituted chalcones: a new class of MAO-B, AChE, and BACE-1 inhibitors for the treatment of neurological disorders. Piperazine 0-10 beta-secretase 1 Homo sapiens 66-72 33668396-1 2021 We have designed and synthesized a series of 60 new 5- and 7-hydroxycoumarin derivatives bearing the piperazine moiety with the expected binding to 5-HT1A and 5-HT2A receptors. Piperazine 101-111 5-hydroxytryptamine receptor 1A Homo sapiens 148-154 33668396-1 2021 We have designed and synthesized a series of 60 new 5- and 7-hydroxycoumarin derivatives bearing the piperazine moiety with the expected binding to 5-HT1A and 5-HT2A receptors. Piperazine 101-111 5-hydroxytryptamine receptor 2A Homo sapiens 161-165 33319990-4 2021 While several derivatives showed low nanomolar antiplasmodium activity (IC50 < 100 nM), some compounds, including piperazine analogue 28, resulted in strong dual PI4K and PKG inhibition. Piperazine 114-124 protein kinase cGMP-dependent 1 Homo sapiens 171-174 32986914-3 2021 Herein we show that such ring systems can be useful for medicinal chemistry at the example of the enantioselective synthesis of triquinazine, a novel chiral piperazine analog derived from angular triquinane, and it"s use to design a nanomolar and selective inhibitor of Janus Kinase 1 related to the marketed drug Tofacitinib useful to treat auto-immune diseases. Piperazine 157-167 Janus kinase 1 Homo sapiens 270-284 33189994-1 2020 In this study, various N-heterocyclic nitro prodrugs (NHN1-16) containing pyrimidine, triazine and piperazine rings were designed and synthesized. Piperazine 99-109 zinc finger CCCH-type containing 18 Homo sapiens 54-58 32947229-0 2020 Structure-activity relationships for a series of (Bis(4-fluorophenyl)methyl)sulfinylethyl-aminopiperidines and -piperidine amines at the dopamine transporter: Bioisosteric replacement of the piperazine improves metabolic stability. Piperazine 191-201 solute carrier family 6 member 3 Homo sapiens 137-157 33837735-6 2021 The 2.3-A crystal structure of Mtb PheRS in complex with PF-3845 revealed its novel binding mode, in which a trifluoromethyl-pyridinylphenyl group occupies the phenylalanine pocket, whereas a piperidine-piperazine urea group binds into the ATP pocket through an interaction network enforced by a sulfate ion. Piperazine 203-213 phenylalanyl-tRNA synthetase subunit beta Homo sapiens 35-40 33397709-6 2021 The 2.3-A crystal structure of Mtb PheRS in complex with PF-3845 revealed its novel binding mode, in which a trifluoromethyl-pyridinylphenyl group occupies the Phe pocket while a piperidine-piperazine urea group binds into the ATP pocket through an interaction network enforced by a sulfate ion. Piperazine 190-200 phenylalanyl-tRNA synthetase subunit beta Homo sapiens 35-40 33052508-4 2021 In response to solubility changes in water/tetrahydrofuran mixtures, while the piperazine bdk ligand showed aggregation caused quenching, the piperidine and morpholine bdks displayed enhanced emission upon aggregation. Piperazine 79-89 kininogen 1 Homo sapiens 90-93 33260358-4 2020 The HL1 ligand results from the condensation of salicylaldehyde and 1-(2-aminoethyl)piperazine, while a new organic ligand, H2L2, was formed by the dimerization of HL1 via a coupling of two piperazine rings of HL1 on a carbon atom coming from DMF solvent. Piperazine 84-94 asialoglycoprotein receptor 1 Homo sapiens 4-7 33255358-4 2020 We recently identified a novel chemical series of human-safe piperazine-based brain-penetrant mTORC1-specific inhibitors. Piperazine 61-71 CREB regulated transcription coactivator 1 Mus musculus 94-100 33255358-5 2020 We assayed the piperazine-mTOR binding strength by two biophysical measurements, biolayer interferometry and field-effect biosensing, and these confirmed each other and demonstrated a structure-activity relationship. Piperazine 15-25 mechanistic target of rapamycin kinase Homo sapiens 26-30 32911196-5 2020 Utilizing information from molecular modelling of the hybrids to the anti-apoptotic Bcl-2 protein, we added substructures including phenyl, piperazine, piperidine, and morpholine rings to their frameworks. Piperazine 140-150 BCL2 apoptosis regulator Homo sapiens 84-89 33126415-4 2020 In this article, we have described the structure-activity relationships (SARs) leading to a novel series of potent and selective piperazine and tetrahydroisoquinoline linked 5-phenoxy-2-aminopyridine irreversible inhibitors of BTK. Piperazine 129-139 Bruton agammaglobulinemia tyrosine kinase Mus musculus 227-230 33017311-2 2020 Altering the concentration of piperazine (pip, ancillary ligand) enables control over the dimensionality of the compound by switching between the 0D [H2pip][Hpip][Pr(pydc)3] 4H2O (I) and the 1D {[Pr(pydc)(Hpydc)(H2O)2] 4H2O}n (II) coordination polymer (CP). Piperazine 30-40 PBX homeobox interacting protein 1 Homo sapiens 157-161 32784090-2 2020 In contrast to compounds built around a piperazine core, most of the fused bicyclic diamine bearing analogs prepared exhibited greater potency against rFAAH than the human enzyme. Piperazine 40-50 fatty-acid amide hydrolase-like Rattus norvegicus 151-156 33017311-2 2020 Altering the concentration of piperazine (pip, ancillary ligand) enables control over the dimensionality of the compound by switching between the 0D [H2pip][Hpip][Pr(pydc)3] 4H2O (I) and the 1D {[Pr(pydc)(Hpydc)(H2O)2] 4H2O}n (II) coordination polymer (CP). Piperazine 30-33 PBX homeobox interacting protein 1 Homo sapiens 157-161 32940185-0 2021 Synthesis, Biological Evaluation, and QPLD Studies of Piperazine Derivatives as Potential DPP-IV Inhibitors. Piperazine 54-64 dipeptidyl peptidase 4 Homo sapiens 90-96 32755677-4 2020 These compounds displayed IC50 values in nanomolar range against A549, MCF7, PC3 and HCT116 cell lines, deducing the discovery that piperazine or 4-aminopiperidine is the linker"s best choice to develop EA analogs with highly potent anti-proliferative activities own up to 24 nM. Piperazine 132-142 chromobox 8 Homo sapiens 77-80 32971892-0 2020 Design, Synthesis, In Vitro and In Silico Studies of New Thiazolylhydrazine-Piperazine Derivatives as Selective MAO-A Inhibitors. Piperazine 76-86 monoamine oxidase A Homo sapiens 112-117 32971892-2 2020 Herein, novel series of thiazolylhydrazine-piperazine derivatives were designed, synthesized and evaluated for their MAO-A and -B inhibitory activity. Piperazine 43-53 monoamine oxidase A Homo sapiens 117-129 32711085-0 2020 Novel bis(pyrazole-benzofuran) hybrids possessing piperazine linker: Synthesis of potent bacterial biofilm and MurB inhibitors. Piperazine 50-60 Bis protein Escherichia coli 6-9 32711085-2 2020 Therefore, 1,3-dipolar cycloaddition of this synthon with the appropriate hydrazonyl chlorides afforded a new series of bis(1,3,4-trisubstituted pyrazoles), linked via piperazine moiety. Piperazine 168-178 Bis protein Escherichia coli 120-123 32583524-2 2020 Orbitazine is a derivative of PAC-1 that has substituted the functional group homopiperazine ring with a piperazine ring. Piperazine 82-92 dual specificity phosphatase 2 Homo sapiens 30-35 32940185-10 2021 CONCLUSION: Piperazine derivatives were found to be successful new scaffold as potential DPP-IV inhibitors. Piperazine 12-22 dipeptidyl peptidase 4 Homo sapiens 89-95 32722122-0 2020 Piperazine- and Piperidine-Containing Thiazolo[5,4-d]pyrimidine Derivatives as New Potent and Selective Adenosine A2A Receptor Inverse Agonists. Piperazine 0-10 adenosine A2a receptor Homo sapiens 104-126 32722122-3 2020 Herein, we report on the synthesis and biological evaluation of a new set of piperazine- and piperidine- containing 7-amino-2-(furan-2-yl)thiazolo[5,4-d]pyrimidine derivatives designed as human A2A AR antagonists/inverse agonists. Piperazine 77-87 immunoglobulin kappa variable 2D-29 Homo sapiens 194-197 32695211-8 2020 In addition, both doses of PZE ameliorated the parenchymal degeneration and necrosis in the liver induced by CCl4 administration, which was associated with reduced expressions of cleaved caspase-3, cleaved poly (ADP-ribose) polymerase, nitrotyrosine, and 4-hydroxynonenal by PZE. Piperazine 27-30 caspase 3 Homo sapiens 187-196 32695211-8 2020 In addition, both doses of PZE ameliorated the parenchymal degeneration and necrosis in the liver induced by CCl4 administration, which was associated with reduced expressions of cleaved caspase-3, cleaved poly (ADP-ribose) polymerase, nitrotyrosine, and 4-hydroxynonenal by PZE. Piperazine 27-30 poly(ADP-ribose) polymerase 1 Homo sapiens 206-234 32551016-4 2020 Piperazine 2 was initially identified as a promising CPS1 inhibitor through a high-throughput screening effort. Piperazine 0-10 carbamoyl-phosphate synthase 1 Homo sapiens 53-57 32388435-2 2020 Conjugates with piperazine linked to the substituted salicylaldoxime emerged as efficient reactivators for VX inhibited hAChE. Piperazine 16-26 acetylcholinesterase (Cartwright blood group) Homo sapiens 120-125 32551016-5 2020 Subsequent structure-activity relationship optimization and structure-based drug design led to the discovery of piperazine H3B-616 (25), a potent allosteric inhibitor of CPS1 (IC50 = 66 nM). Piperazine 112-122 carbamoyl-phosphate synthase 1 Homo sapiens 170-174 32125570-6 2020 Theoretical calculations show the possible structure both of the L-beta-CD adduct and of the coordination mode of Al3+ ion to L. In the presence of beta-CD, the piperazine adopts a distorted conformation. Piperazine 161-171 ACD shelterin complex subunit and telomerase recruitment factor Homo sapiens 67-74 32125570-6 2020 Theoretical calculations show the possible structure both of the L-beta-CD adduct and of the coordination mode of Al3+ ion to L. In the presence of beta-CD, the piperazine adopts a distorted conformation. Piperazine 161-171 ACD shelterin complex subunit and telomerase recruitment factor Homo sapiens 148-155 31499259-0 2019 Development of novel chromeno[4,3-c]pyrazol-4(2H)-one derivates containing piperazine as inhibitors of PI3Kalpha. Piperazine 75-85 phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha Homo sapiens 103-112 32202029-5 2020 Finally, utilizing an optimized cocktail of 2% DBU + 5% piperazine for fast Fmoc-deprotection, we report the synthesis of a thioamidated Pin1 WW domain and thioamidated GB1 directly on solid support. Piperazine 56-66 peptidylprolyl cis/trans isomerase, NIMA-interacting 1 Homo sapiens 137-141 32202029-5 2020 Finally, utilizing an optimized cocktail of 2% DBU + 5% piperazine for fast Fmoc-deprotection, we report the synthesis of a thioamidated Pin1 WW domain and thioamidated GB1 directly on solid support. Piperazine 56-66 gamma-aminobutyric acid type B receptor subunit 1 Homo sapiens 169-172 31483229-5 2020 The generated model of alpha 7 nicotinic acetylcholine receptor was used for docking study of 27 piperazine analogues using Auto-Dock 4.2.5.1. Piperazine 97-107 cholinergic receptor nicotinic alpha 7 subunit Homo sapiens 23-63 31421254-6 2019 It is observed that the piperazine scaffold containing compound is more active than the compound with piperidine scaffold for exerting HDAC8 inhibitory activity. Piperazine 24-34 histone deacetylase 8 Homo sapiens 135-140 31374520-0 2019 Sulfonamides incorporating piperazine bioisosteres as potent human carbonic anhydrase I, II, IV and IX inhibitors. Piperazine 27-37 carbonic anhydrase 1 Homo sapiens 67-87 31390199-5 2019 Therefore, clarifying the binding mode between PPARgamma and small molecules, we focused on the introduction of a natural active piperazine skeleton in the position of glycyrrhetinic acid C-3. Piperazine 129-139 peroxisome proliferator activated receptor gamma Homo sapiens 47-56 30764944-1 2019 Fe3O4@MCM-41@Zirconium magnetic nanoparticles modified with piperazine (Fe3O4@MCM-41@Zr-piperazine), as a newly reported catalyst, shows excellent catalytic activity in N-Tert-butoxycarbonylation of amines under the mild and solvent-free conditions. Piperazine 60-70 telomerase reverse transcriptase Homo sapiens 171-175 31118272-8 2019 The RET-nintedanib co-crystal structure disclosed that Leu-730 in RET engages in hydrophobic interactions with the piperazine, anilino, and phenyl groups of nintedanib, providing a structural basis for explaining that the p.L730V mutation identified in nine independently isolated cell lines resistant to nintedanib. Piperazine 115-125 ret proto-oncogene Homo sapiens 4-7 31118272-8 2019 The RET-nintedanib co-crystal structure disclosed that Leu-730 in RET engages in hydrophobic interactions with the piperazine, anilino, and phenyl groups of nintedanib, providing a structural basis for explaining that the p.L730V mutation identified in nine independently isolated cell lines resistant to nintedanib. Piperazine 115-125 ret proto-oncogene Homo sapiens 66-69 30764944-1 2019 Fe3O4@MCM-41@Zirconium magnetic nanoparticles modified with piperazine (Fe3O4@MCM-41@Zr-piperazine), as a newly reported catalyst, shows excellent catalytic activity in N-Tert-butoxycarbonylation of amines under the mild and solvent-free conditions. Piperazine 88-98 telomerase reverse transcriptase Homo sapiens 171-175 31117309-0 2019 Three-Dimensional Quantitative Structure-Activity Relationships (3D-QSAR) on a Series of Piperazine-Carboxamides Fatty Acid Amide Hydrolase (FAAH) Inhibitors as a Useful Tool for the Design of New Cannabinoid Ligands. Piperazine 89-99 fatty acid amide hydrolase Homo sapiens 141-145 31173031-3 2019 Our series of 33 novel compounds contain the CA-4 core structure with modifications to the stilbene linking group, and are predominantly piperazine derivatives. Piperazine 137-147 carbonic anhydrase 4 Homo sapiens 45-49 31117309-3 2019 In the present work, we present a three-dimensional quantitative structure-activity relationships/comparative molecular similarity indices analysis (3D-QSAR/CoMSIA) study on a series of 90 reported irreversible inhibitors of FAAH sharing a piperazine-carboxamide scaffold. Piperazine 240-250 fatty acid amide hydrolase Homo sapiens 225-229 30608334-1 2019 This study was designed to characterize the pharmacological profile of DS37001789, which is a structurally novel piperazine derivative that acts as urotensin II (U-II) receptor antagonist. Piperazine 113-123 urotensin 2 Homo sapiens 148-160 30689993-6 2019 The piperazine agonist 1-(3-chlorophenyl)piperazine (mCPP), with lower potency but similar efficacy as 5-HT, elicited desensitization indistinguishable from 5-HT, while the piperazine agonist aripiprazole, with lower potency and efficacy, did not desensitize 5-HT2C-PLC signaling. Piperazine 4-14 5-hydroxytryptamine receptor 2C Homo sapiens 259-265 30689993-6 2019 The piperazine agonist 1-(3-chlorophenyl)piperazine (mCPP), with lower potency but similar efficacy as 5-HT, elicited desensitization indistinguishable from 5-HT, while the piperazine agonist aripiprazole, with lower potency and efficacy, did not desensitize 5-HT2C-PLC signaling. Piperazine 41-51 5-hydroxytryptamine receptor 2C Homo sapiens 259-265 30696719-10 2019 In agreement with previously published data, we have shown that PPZ potentiates TRPC6 channels. Piperazine 64-67 transient receptor potential cation channel, subfamily C, member 6 Mus musculus 80-85 30622024-11 2019 Therefore, these results suggest that piperazine moiety is essential for dual activity (PAM & NAM) of compounds 58, and supports the hypothesis of 5-HT2C PAM for the treatment of obesity similar to the full agonist. Piperazine 38-48 5-hydroxytryptamine receptor 2C Rattus norvegicus 151-157 30605887-0 2019 Biphenyl-3-oxo-1,2,4-triazine linked piperazine derivatives as potential cholinesterase inhibitors with anti-oxidant property to improve the learning and memory. Piperazine 37-47 acetylcholinesterase Mus musculus 73-87 30622024-0 2019 Identification of dual role of piperazine-linked phenyl cyclopropyl methanone as positive allosteric modulator of 5-HT2C and negative allosteric modulator of 5-HT2B receptors. Piperazine 31-41 5-hydroxytryptamine receptor 2C Rattus norvegicus 114-120 30622024-0 2019 Identification of dual role of piperazine-linked phenyl cyclopropyl methanone as positive allosteric modulator of 5-HT2C and negative allosteric modulator of 5-HT2B receptors. Piperazine 31-41 5-hydroxytryptamine receptor 2B Rattus norvegicus 158-164 30622024-6 2019 Interestingly, piperazine linked phenyl cyclopropyl methanones (58) was active as PAM of 5-HT2C (increased the Emax of 5-HT to 139%), and as negative allosteric modulator (NAM) of 5-HT2B (decreases EC50 of 5-HT 10 times without affecting Emax). Piperazine 15-25 5-hydroxytryptamine receptor 2C Rattus norvegicus 89-95 30622024-6 2019 Interestingly, piperazine linked phenyl cyclopropyl methanones (58) was active as PAM of 5-HT2C (increased the Emax of 5-HT to 139%), and as negative allosteric modulator (NAM) of 5-HT2B (decreases EC50 of 5-HT 10 times without affecting Emax). Piperazine 15-25 5-hydroxytryptamine receptor 2B Rattus norvegicus 180-186 30626065-3 2019 In this study, we investigated the effects of several piperazine derivatives on P-gp function in vitro. Piperazine 54-64 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 80-84 30626065-9 2019 A piperazine derivative, compound 4, which was confirmed as a substantial P-gp inhibitor in vitro increased the BA of PTX up to 2-fold by a lingering absorption, in part due to inhibition of intestinal P-gp and a low oral clearance of PTX. Piperazine 2-12 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 74-78 30626065-9 2019 A piperazine derivative, compound 4, which was confirmed as a substantial P-gp inhibitor in vitro increased the BA of PTX up to 2-fold by a lingering absorption, in part due to inhibition of intestinal P-gp and a low oral clearance of PTX. Piperazine 2-12 ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus 202-206 30028993-8 2018 By contrast, the piperazine drug cinnarizine dose-dependently inhibited mTORC1 but not mTORC2, suggesting it as a novel mTORC1-specific inhibitor. Piperazine 17-27 CREB regulated transcription coactivator 1 Mus musculus 72-78 30010318-3 2018 Our goal was to investigate how the composition and size of the nonaromatic ring structure at the piperazine position of substituted phenylpiperazine analogues might influence binding affinity at the human D2 and D3 dopamine receptors. Piperazine 98-108 dopamine receptor D2 Homo sapiens 206-234 30456211-7 2018 Complex 1 shows catalase activity only in the presence of a base, e.g., piperazine or triethylamine. Piperazine 72-82 catalase Homo sapiens 16-24 30106271-4 2018 Upon complexation, the conformation of piperazine fragment changes from chair to boat in which the triazole and piperazine units create a cavity to tether Cr3+. Piperazine 39-49 teratocarcinoma-derived growth factor 1 pseudogene 3 Homo sapiens 155-158 30106271-4 2018 Upon complexation, the conformation of piperazine fragment changes from chair to boat in which the triazole and piperazine units create a cavity to tether Cr3+. Piperazine 112-122 teratocarcinoma-derived growth factor 1 pseudogene 3 Homo sapiens 155-158 30028993-8 2018 By contrast, the piperazine drug cinnarizine dose-dependently inhibited mTORC1 but not mTORC2, suggesting it as a novel mTORC1-specific inhibitor. Piperazine 17-27 CREB regulated transcription coactivator 1 Mus musculus 120-126 30028993-11 2018 Since mTOR inhibition is a general anti-cancer strategy, and mTORC1 is specifically activated in some tumors, we suggest the piperazine scaffold, including cinnarizine and hydroxyzine, could be proposed for rational therapy in tumors in which mTORC1 is specifically activated. Piperazine 125-135 mechanistic target of rapamycin kinase Homo sapiens 6-10 30028993-11 2018 Since mTOR inhibition is a general anti-cancer strategy, and mTORC1 is specifically activated in some tumors, we suggest the piperazine scaffold, including cinnarizine and hydroxyzine, could be proposed for rational therapy in tumors in which mTORC1 is specifically activated. Piperazine 125-135 CREB regulated transcription coactivator 1 Mus musculus 61-67 30028993-11 2018 Since mTOR inhibition is a general anti-cancer strategy, and mTORC1 is specifically activated in some tumors, we suggest the piperazine scaffold, including cinnarizine and hydroxyzine, could be proposed for rational therapy in tumors in which mTORC1 is specifically activated. Piperazine 125-135 CREB regulated transcription coactivator 1 Mus musculus 243-249 30028993-13 2018 Thus piperazine-based mTOR inhibitors could become a novel chemotherapeutic strategy. Piperazine 5-15 mechanistic target of rapamycin kinase Homo sapiens 22-26 29519733-1 2018 Exploration of alternative structures of the substituted piperidine or piperazine ring which are characteristic in most of the reported GPR119 agonists provided novel spirocyclic cyclohexane derivatives. Piperazine 71-81 G protein-coupled receptor 119 Rattus norvegicus 136-142 29677541-0 2018 Tert-butyl 4-((1-phenyl-1H-pyrazol-4-yl) methyl) piperazine-1-carboxylate (LQFM104)- New piperazine derivative with antianxiety and antidepressant-like effects: Putative role of serotonergic system. Piperazine 49-59 telomerase reverse transcriptase Mus musculus 0-4 29579709-0 2018 The novel piperazine-containing compound LQFM018: Necroptosis cell death mechanisms, dopamine D4 receptor binding and toxicological assessment. Piperazine 10-20 dopamine receptor D4 Homo sapiens 85-105 30049229-0 2018 Highly selective N-glucuronidation of four piperazine-containing drugs by UDP-glucuronosyltransferase 2B10. Piperazine 43-53 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 74-106 30049229-9 2018 CONCLUSIONS: UGT2B10 plays a critical role in N-glucuronidation of piperazine-containing drugs. Piperazine 67-77 UDP glucuronosyltransferase family 2 member B10 Homo sapiens 13-20 29635165-3 2018 One of the compounds, 8, containing a terminal piperazine appendage with a carboxamide moiety at position 8 and phenyl group at position 9 of 6-chloro-8,9-dihydro-7H-purine core, showed the most potent antiproliferative activity and good selectivity between cancer and normal cells (IC50 values of 2.80 muM against A549 and 303.03 muM against GES-1, respectively). Piperazine 47-57 latexin Homo sapiens 303-306 29635165-3 2018 One of the compounds, 8, containing a terminal piperazine appendage with a carboxamide moiety at position 8 and phenyl group at position 9 of 6-chloro-8,9-dihydro-7H-purine core, showed the most potent antiproliferative activity and good selectivity between cancer and normal cells (IC50 values of 2.80 muM against A549 and 303.03 muM against GES-1, respectively). Piperazine 47-57 latexin Homo sapiens 331-334 29299575-2 2018 The piperazine-based ligands were designed to be potential inhibitors of GSK-3beta kinase. Piperazine 4-14 glycogen synthase kinase 3 beta Homo sapiens 73-82 29324250-0 2018 Novel sulfonamide incorporating piperazine, aminoalcohol and 1,3,5-triazine structural motifs with carbonic anhydrase I, II and IX inhibitory action. Piperazine 32-42 carbonic anhydrase 1 Homo sapiens 99-119 29287256-0 2018 A simple and efficient synthesis of benzimidazoles containing piperazine or morpholine skeleton at C-6 position as glucosidase inhibitors with antioxidant activity. Piperazine 62-72 complement C6 Homo sapiens 99-102 29421572-6 2018 The results of all pharmacological assays indicated that the combination of a basic piperazine scaffold with arylalkyl residues allowed us to obtain very interesting P-gp modulating compounds. Piperazine 84-94 phosphoglycolate phosphatase Homo sapiens 166-170 29269256-4 2018 Compound 6a and 10a bearing a bromo- or methoxy- substituent in ortho position of the piperazine phenyl ring, were identified as potent antagonists of the 5-HT1A receptors. Piperazine 86-96 5-hydroxytryptamine (serotonin) receptor 1A Mus musculus 155-161 30047333-0 2018 2D & 3D-QSAR Study on Novel Piperidine and Piperazine Derivatives as Acetylcholinesterase Enzyme Inhibitors. Piperazine 43-53 acetylcholinesterase (Cartwright blood group) Homo sapiens 69-96 30026636-5 2017 The method described here enables the incorporation of late-stage structural diversity into diaryl sulfides containing the piperazine ring, thus enhancing the number and nature of derivatives available for SAR investigation. Piperazine 123-133 sarcosine dehydrogenase Homo sapiens 206-209 29173145-0 2018 Histamine H3 Receptor Ligands in the Group of (Homo)piperazine Derivatives. Piperazine 52-62 histamine receptor H3 Homo sapiens 0-21 29173145-3 2018 One such replacement is piperazine moiety, a significant versatile scaffold in rational drug design for most of the GPCR ligands. Piperazine 24-34 G protein-coupled receptor 166 pseudogene Homo sapiens 116-120 29205121-6 2018 CONCLUSION: Docking into the oncogenic kinase bcr/abl illustrated the critical importance of (i) phalogen substituent on the ligand"s phenyl ring and (ii) the presence of positive ionizable moiety at the ligand"s piperazine fragment for anticancer activity. Piperazine 213-223 BCR activator of RhoGEF and GTPase Homo sapiens 46-49 29153425-0 2017 Fluoroethoxy-1,4-diphenethylpiperidine and piperazine derivatives: Potent and selective inhibitors of [3H]dopamine uptake at the vesicular monoamine transporter-2. Piperazine 43-53 solute carrier family 18 member A2 Homo sapiens 129-162 29132093-0 2017 A benzothiazole/piperazine derivative with acetylcholinesterase inhibitory activity: Improvement in streptozotocin-induced cognitive deficits in rats. Piperazine 16-26 acetylcholinesterase Rattus norvegicus 43-63 28925739-2 2017 Materials & methods: Piperazine-based thiazolidinones were synthesized and screened for their anticancer and VEGFR2 tyrosine kinase inhibitory activity. Piperazine 25-35 kinase insert domain receptor Homo sapiens 113-119 28803048-3 2017 alpha,beta-Unsaturated glycyrrhetic acids showed better activity, among them, compounds 6k and 6l with piperazine unit exhibited the most potent nitric oxide (NO) and interleukin-6 (IL-6) inhibitory activity (IC50 = 13.3 and 15.5 muM respectively). Piperazine 103-113 interleukin 6 Mus musculus 182-186 29036189-0 2017 Inhibition of CUG-binding protein 1 and activation of caspases are critically involved in piperazine derivative BK10007S induced apoptosis in hepatocellular carcinoma cells. Piperazine 90-100 caspase 8 Homo sapiens 54-62 28751116-5 2017 This cooperative metabolic pathway by MAO-B and AO was newly identified in the metabolism of piperazine. Piperazine 93-103 monoamine oxidase B Homo sapiens 38-43 29046637-3 2017 As an agonist of PXR, meclizine is a piperazine-derived histamine H1 antagonist, and has been frequently used for prevention and treatment of vomiting and nausea. Piperazine 37-47 nuclear receptor subfamily 1 group I member 2 Homo sapiens 17-20 28363444-0 2017 Discovery of a series of 1,3,4-oxadiazole-2(3H)-thione derivatives containing piperazine skeleton as potential FAK inhibitors. Piperazine 78-88 protein tyrosine kinase 2 Homo sapiens 111-114 28712706-2 2017 Transformation of the morpholine moiety into a piperazine moiety resulted in potent GSK-3beta inhibitors. Piperazine 47-57 glycogen synthase kinase 3 beta Mus musculus 84-93 28712706-3 2017 SAR studies focused on the nitrogen atom of the piperazine moiety revealed that a phenyl group afforded potent inhibitory activity toward GSK-3beta. Piperazine 48-58 glycogen synthase kinase 3 beta Mus musculus 138-147 28712706-4 2017 Docking studies indicated that the phenyl group on the piperazine nitrogen atom and the methyl group on the piperazine make cation-pi and CH-pi interactions with GSK-3beta respectively. Piperazine 55-65 glycogen synthase kinase 3 beta Mus musculus 162-171 28712706-4 2017 Docking studies indicated that the phenyl group on the piperazine nitrogen atom and the methyl group on the piperazine make cation-pi and CH-pi interactions with GSK-3beta respectively. Piperazine 108-118 glycogen synthase kinase 3 beta Mus musculus 162-171 28712708-2 2017 Transformation of the morpholine moiety into a piperazine moiety resulted in potent GSK-3beta inhibitors. Piperazine 47-57 glycogen synthase kinase 3 beta Homo sapiens 84-93 28409931-1 2017 We have designed and synthesized novel piperazine compounds with low lipophilicity as sigma1 receptor ligands. Piperazine 39-49 sigma non-opioid intracellular receptor 1 Mus musculus 86-101 28363444-2 2017 We report herein the discovery of a novel class of 1,3,4-oxadiazole-2(3H)-thione derivatives containing piperazine skeleton with improved potency toward FAK. Piperazine 104-114 protein tyrosine kinase 2 Homo sapiens 153-156 28366621-4 2017 Using a phenotypic screening strategy, we identified a series of piperazine phenothiazines, including trifluoperazine, which rescued Pink1 deficiency by activating autophagy selectively in stressed zebrafish and human cells. Piperazine 65-75 PTEN induced kinase 1 Danio rerio 133-138 27786487-1 2016 The stereocontrolled synthesis of a range of substituted bicyclic morpholine and piperazine derivatives is reported from substituted pyroglutaminols via an intramolecular SN2 cyclization as the key step. Piperazine 81-91 solute carrier family 38 member 5 Homo sapiens 171-174 28165094-3 2017 On the other hand, the presence of the piperazine moiety on the bay position of the PDI core makes it an ideal electron donor, nicely coupled with the electron accepting exfoliated graphene, hence, forming a novel donor-acceptor nanoensemble, which was characterized by complementary spectroscopic and microscopy techniques. Piperazine 39-49 peptidyl arginine deiminase 1 Homo sapiens 84-87 27721153-3 2017 In vitro studies showed that the majority of saccharin derivatives with piperazine moiety and one phthalimide derivative with 3-aminopiperidine fragment exhibited inhibitory potency toward acetylcholinesterase (AChE) with EeAChE IC50 values ranging from 0.83 muM to 19.18 muM. Piperazine 72-82 acetylcholinesterase (Cartwright blood group) Homo sapiens 211-215 27810598-0 2017 In silico identification, design and synthesis of novel piperazine-based antiviral agents targeting the hepatitis C virus helicase. Piperazine 56-66 helicase for meiosis 1 Homo sapiens 122-130 28219076-1 2017 BACKGROUND: N-benzylpiperazine (BZP) belongs to a class of piperazine derivatives (PZDs) that have emerged as recreational drugs. Piperazine 59-81 zinc finger E-box binding homeobox 1 Mus musculus 12-30 28219076-1 2017 BACKGROUND: N-benzylpiperazine (BZP) belongs to a class of piperazine derivatives (PZDs) that have emerged as recreational drugs. Piperazine 59-81 zinc finger E-box binding homeobox 1 Mus musculus 32-35 28219076-1 2017 BACKGROUND: N-benzylpiperazine (BZP) belongs to a class of piperazine derivatives (PZDs) that have emerged as recreational drugs. Piperazine 83-87 zinc finger E-box binding homeobox 1 Mus musculus 12-30 28219076-1 2017 BACKGROUND: N-benzylpiperazine (BZP) belongs to a class of piperazine derivatives (PZDs) that have emerged as recreational drugs. Piperazine 83-87 zinc finger E-box binding homeobox 1 Mus musculus 32-35 26821219-9 2016 Key enzymes of cholesterol biosynthesis up-regulated by all four piperazine drugs include sterol C4-methyloxidase, isopentyl-diphosphate-Delta-isomerase, Cyp51A1, squalene epoxidase and farnesyl diphosphate synthase. Piperazine 65-75 cytochrome P450, family 51 Rattus norvegicus 154-161 26821219-9 2016 Key enzymes of cholesterol biosynthesis up-regulated by all four piperazine drugs include sterol C4-methyloxidase, isopentyl-diphosphate-Delta-isomerase, Cyp51A1, squalene epoxidase and farnesyl diphosphate synthase. Piperazine 65-75 squalene epoxidase Rattus norvegicus 163-181 26821219-9 2016 Key enzymes of cholesterol biosynthesis up-regulated by all four piperazine drugs include sterol C4-methyloxidase, isopentyl-diphosphate-Delta-isomerase, Cyp51A1, squalene epoxidase and farnesyl diphosphate synthase. Piperazine 65-75 farnesyl diphosphate synthase Rattus norvegicus 186-215 26821219-10 2016 Additionally, glycoprotein transmembrane nmb, which participates in cell adhesion processes, and fatty acid desaturase 1, an enzyme that regulates unsaturation of fatty acids, were also up-regulated by the four piperazine designer drugs. Piperazine 211-221 fatty acid desaturase 1 Rattus norvegicus 97-120 26821219-11 2016 Regarding the down-regulated probe sets, only one gene was common to all four piperazine derivatives, the betaine-homocysteine-S-methyltransferase 2. Piperazine 78-88 betaine-homocysteine S-methyltransferase 2 Rattus norvegicus 106-148 26821219-12 2016 Analysis of transcription factor binding sites of the "piperazine designer drug consensus signature" identified the sterol regulatory element binding protein (SREBP-1) as strongly overrepresented in the up-regulated genes. Piperazine 55-65 sterol regulatory element binding transcription factor 1 Rattus norvegicus 159-166 27287367-3 2016 The conformationally restricted piperazine derivative 19 and the oxamide-derived bisbenzamidine 1 were identified as the most potent inhibitors of this series for matriptase-2 and matriptase, respectively. Piperazine 32-42 transmembrane serine protease 6 Homo sapiens 163-190 27479541-2 2016 This biological study showed that these compounds containing piperazine ring had significant inhibition activities on AChE rather than BuChE. Piperazine 61-71 butyrylcholinesterase Homo sapiens 135-140 27448915-2 2016 Most synthesized compounds presented improved antiproliferative activities compared to the parent bile acids (IC50 > 80 muM), especially the piperazine conjugated compound 27 with IC50 values of 1.07, 4.58 and 3.86 muM against PC3M, HT29 and ES-2 cancer cell lines, respectively. Piperazine 144-154 latexin Homo sapiens 218-221 27102880-4 2016 We recently found that EVT901, a novel piperazine derivative that inhibits p75NTR oligomerization, is neuroprotective, reduces microglial activation, and improves outcomes in two models of TBI in rats. Piperazine 39-49 nerve growth factor receptor Rattus norvegicus 75-81 27493695-10 2016 The binding interactions of the ligand molecules, with piperazine moiety as a pharmacophore, are observed at Arg67 and Glu149 residues of the FGF-7 protein. Piperazine 55-65 fibroblast growth factor 7 Homo sapiens 142-147 26714831-0 2016 Synthesis of Novel Pyrimidin-4-One Bearing Piperazine Ring-Based Amides as Glycogen Synthase Kinase-3beta Inhibitors with Antidepressant Activity. Piperazine 43-53 glycogen synthase kinase 3 beta Homo sapiens 75-105 27092414-0 2016 Syntheses, biological activities and SAR studies of novel carboxamide compounds containing piperazine and arylsulfonyl moieties. Piperazine 91-101 sarcosine dehydrogenase Homo sapiens 37-40 26990539-4 2016 Starting with a crystal structure of LXRbeta and a docked 2-(methylsulfonyl)benzyl alcohol fragment (6), Contour was used to design agonists containing a piperazine core. Piperazine 154-164 nuclear receptor subfamily 1 group H member 2 Homo sapiens 37-44 27072064-1 2016 The current study evaluates the cytotoxic mechanism of a novel piperazine derivate designated as PCC against human liver cancer cells. Piperazine 63-73 crystallin gamma D Homo sapiens 97-100 26943020-5 2016 Piperazine residues at position 4 bearing large phenylalkyl side chains proved to be beneficial for MRP1 inhibition. Piperazine 0-10 ATP binding cassette subfamily C member 1 Homo sapiens 100-104 27134115-4 2016 We have found that compounds with a hydroxyl group at C-4 of the aryl ring on the piperazine moiety possess Hsp90 inhibition properties. Piperazine 82-92 heat shock protein 90 alpha family class A member 1 Homo sapiens 108-113 25987376-1 2015 A series of new fluorescent symmetric dimeric bisbenzimidazoles DBP(n) bearing bisbenzimidazole fragments joined by oligomethylene linkers with a central 1,4-piperazine residue were synthesized. Piperazine 154-168 D-box binding PAR bZIP transcription factor Homo sapiens 64-67 27941264-6 2016 Linearity, accuracy, and precision were found to be acceptable over the piperazine concentration range of 0.3525 - 2.35 ng mL-1. Piperazine 72-82 L1 cell adhesion molecule Mus musculus 123-127 27941264-7 2016 The limit of detection and limit of quantification of piperazine were 0.1175 and 0.3525 ng mL-1, respectively, which complied with the requirements of qualitative and quantitative analyses. Piperazine 54-64 L1 cell adhesion molecule Mus musculus 91-95 26483200-1 2015 The present study describes the optimization of a series of novel benzoxazole-piperidine (piperazine) derivatives combining high dopamine D2 and serotonin 5-HT1A, 5-HT2A receptor affinities. Piperazine 90-100 immunoglobulin heavy diversity 2-15 Homo sapiens 138-161 26483200-1 2015 The present study describes the optimization of a series of novel benzoxazole-piperidine (piperazine) derivatives combining high dopamine D2 and serotonin 5-HT1A, 5-HT2A receptor affinities. Piperazine 90-100 5-hydroxytryptamine receptor 2A Homo sapiens 163-178 25906763-2 2015 The binding of piperazine derivative to bovine serum albumin (BSA) was investigated using fluorescence spectroscopy. Piperazine 15-25 albumin Homo sapiens 47-60 27019772-1 2016 The purpose of this study was to assess the cytotoxic potential of a novel piperazine derivative (PCC) against human liver cancer cells. Piperazine 75-85 crystallin gamma D Homo sapiens 98-101 26733543-4 2016 We discovered, through library screening, a group of piperazine-derived compounds that activate DAG-activated TRPC3/TRPC6/TRPC7 channels. Piperazine 53-63 transient receptor potential cation channel subfamily C member 3 Homo sapiens 110-115 26733543-4 2016 We discovered, through library screening, a group of piperazine-derived compounds that activate DAG-activated TRPC3/TRPC6/TRPC7 channels. Piperazine 53-63 transient receptor potential cation channel subfamily C member 6 Homo sapiens 116-121 26733543-4 2016 We discovered, through library screening, a group of piperazine-derived compounds that activate DAG-activated TRPC3/TRPC6/TRPC7 channels. Piperazine 53-63 transient receptor potential cation channel subfamily C member 7 Homo sapiens 122-127 26832218-4 2016 The synthesis and SAR of these substituted piperidine and piperazine CGRP antagonists are discussed. Piperazine 58-68 sarcosine dehydrogenase Homo sapiens 18-21 26832218-4 2016 The synthesis and SAR of these substituted piperidine and piperazine CGRP antagonists are discussed. Piperazine 58-68 calcitonin related polypeptide alpha Homo sapiens 69-73 26547056-2 2015 Various modifications at the 4-position of the piperazine moiety of the new lead compound were performed to improve P2X7 receptor antagonistic activities, which were evaluated in HEK293 cells stably expressing the human P2X7 receptor (EtBr uptake assay) and in THP-1 cells (IL-1beta ELISA assay). Piperazine 47-57 purinergic receptor P2X 7 Homo sapiens 116-129 25936257-1 2015 Synthetic routes to six 3-D scaffolds containing piperazine, pyrrolidine and piperidine cores have been developed. Piperazine 49-59 SIX homeobox 3 Homo sapiens 20-25 25282655-0 2014 Piperazine and piperidine carboxamides and carbamates as inhibitors of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL). Piperazine 0-10 fatty acid amide hydrolase Homo sapiens 71-97 25712164-3 2015 In this study, we used a RNA aptamer against EpCAM (EpDT3) attached physically to our newly synthesized non-viral vector, based on single-walled carbon nanotube (SWNT) conjugated to piperazine-polyethylenimine derivative. Piperazine 182-192 epithelial cell adhesion molecule Homo sapiens 45-50 25267303-6 2015 In examples of the SUOX-fold and DMSOR-fold enzymes, we observe three types of histidine-containing charge-transfer relays that can: (1) connect the piperazine ring of the pyranopterin to the substrate-binding site (SUOX-fold enzymes); (2) provide inter-pyranopterin communication (DMSOR-fold enzymes); and (3) connect a pyran ring oxygen to deeply buried water molecules (the DMSOR-fold NarGHI-type nitrate reductases). Piperazine 149-159 sulfite oxidase Homo sapiens 19-23 25267303-6 2015 In examples of the SUOX-fold and DMSOR-fold enzymes, we observe three types of histidine-containing charge-transfer relays that can: (1) connect the piperazine ring of the pyranopterin to the substrate-binding site (SUOX-fold enzymes); (2) provide inter-pyranopterin communication (DMSOR-fold enzymes); and (3) connect a pyran ring oxygen to deeply buried water molecules (the DMSOR-fold NarGHI-type nitrate reductases). Piperazine 149-159 sulfite oxidase Homo sapiens 216-220 25216392-0 2015 Design, synthesis, biological screening, and molecular docking studies of piperazine-derived constrained inhibitors of DPP-IV for the treatment of type 2 diabetes. Piperazine 74-84 dipeptidylpeptidase 4 Mus musculus 119-125 25216392-1 2015 Novel piperazine-derived conformationally constrained compounds were designed, synthesized, and evaluated for in vitro Dipeptidyl peptidase-IV (DPP-IV) inhibitory activities. Piperazine 6-16 dipeptidylpeptidase 4 Mus musculus 119-142 25216392-1 2015 Novel piperazine-derived conformationally constrained compounds were designed, synthesized, and evaluated for in vitro Dipeptidyl peptidase-IV (DPP-IV) inhibitory activities. Piperazine 6-16 dipeptidylpeptidase 4 Mus musculus 144-150 25240828-7 2015 The presence of CH2 stretching modes in the SERS spectrum indicates the close of piperazine ring with the metal surface and the interaction of the silver surface with this moiety. Piperazine 81-91 seryl-tRNA synthetase 2, mitochondrial Homo sapiens 44-48 25282655-0 2014 Piperazine and piperidine carboxamides and carbamates as inhibitors of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL). Piperazine 0-10 fatty acid amide hydrolase Homo sapiens 99-103 25282655-0 2014 Piperazine and piperidine carboxamides and carbamates as inhibitors of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL). Piperazine 0-10 monoglyceride lipase Homo sapiens 109-132 25282655-0 2014 Piperazine and piperidine carboxamides and carbamates as inhibitors of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL). Piperazine 0-10 monoglyceride lipase Homo sapiens 134-138 25282655-2 2014 In this paper, we present more extensively the results of our previous work on piperazine and piperidine carboxamides and carbamates as FAAH and MAGL inhibitors. Piperazine 79-89 fatty acid amide hydrolase Homo sapiens 136-140 25282655-2 2014 In this paper, we present more extensively the results of our previous work on piperazine and piperidine carboxamides and carbamates as FAAH and MAGL inhibitors. Piperazine 79-89 monoglyceride lipase Homo sapiens 145-149 25273356-0 2014 Mechanism-based inactivation of human cytochrome P450 3A4 by two piperazine-containing compounds. Piperazine 65-75 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 38-57 25311421-13 2014 Two of the new piperaquine phosphate related substances, imp-2 and imp-6, were identified and characterized as 4-hydroxy-7-chloro-quinoline and a piperaquine oxygenate with a piperazine ring of nitrogen oxide in bulk drug and oxidation sample, respectively. Piperazine 175-185 inositol monophosphatase 2 Homo sapiens 57-62 24880238-7 2014 Piperazine derivatived from betulinic acid presented minimum inhibitory concentration (MIC) value of 91.2 muM, and the kinetic growth curve performed with parasites treated with this most active compound revealed complete inhibition of trophozoite proliferation at 2 h of incubation and total abolition of trophozoite growth in 24 h, revealing that the piperazine derivative is an efficient trichomonacidal molecule. Piperazine 0-10 latexin Homo sapiens 106-109 24856182-0 2014 Combination of cyclohexane and piperazine based kappa-opioid receptor agonists: Synthesis and pharmacological evaluation of trans,trans-configured perhydroquinoxalines. Piperazine 31-41 opioid receptor kappa 1 Homo sapiens 48-69 24731275-0 2014 Design, syntheses, and characterization of piperazine based chemokine receptor CCR5 antagonists as anti prostate cancer agents. Piperazine 43-53 C-C motif chemokine receptor 5 Homo sapiens 79-83 24991704-0 2014 Synthesis and labeling of a piperazine-based library of 11C-labeled ligands for imaging of the vesicular acetylcholine transporter. Piperazine 28-38 solute carrier family 18 member A3 Homo sapiens 95-130 24991704-8 2014 To conclude, a general method for a facile synthesis and labeling of a small piperazine-based library of potential PET tracers for imaging of VAChT was shown, and in upcoming work, another scaffold will be explored using this approach. Piperazine 77-87 solute carrier family 18 member A3 Homo sapiens 142-147 24743647-5 2014 Whole-cell recordings reveal that GABA, muscimol and the anthelmintic piperazine elicit macroscopic currents from UNC-49 receptors that decay in their sustained presence, indicating full desensitization. Piperazine 70-80 Neur_chan_LBD domain-containing protein;Neur_chan_memb domain-containing protein;Uncharacterized protein Caenorhabditis elegans 114-120 24365161-1 2014 In this letter, we describe a series of 4-substituted piperidine and piperazine compounds based on tetrahydroquinoline 1, a compound that shows balanced, low nanomolar binding affinity for the mu opioid receptor (MOR) and the delta opioid receptor (DOR). Piperazine 69-79 opioid receptor mu 1 Homo sapiens 193-211 24201896-4 2014 In general the homopiperazine complexes show higher cytotoxicity than the piperazine complexes, with the most cytotoxic complex exhibiting IC50 (muM) values of 3 +- 0.5 muM (HT-29) and 4 +- 1 muM (OVCAR). Piperazine 19-29 latexin Homo sapiens 145-148 24201896-4 2014 In general the homopiperazine complexes show higher cytotoxicity than the piperazine complexes, with the most cytotoxic complex exhibiting IC50 (muM) values of 3 +- 0.5 muM (HT-29) and 4 +- 1 muM (OVCAR). Piperazine 19-29 latexin Homo sapiens 169-172 24201896-4 2014 In general the homopiperazine complexes show higher cytotoxicity than the piperazine complexes, with the most cytotoxic complex exhibiting IC50 (muM) values of 3 +- 0.5 muM (HT-29) and 4 +- 1 muM (OVCAR). Piperazine 19-29 latexin Homo sapiens 169-172 24502948-0 2014 Piperazine derivatives inhibit PrP/PrP(res) propagation in vitro and in vivo. Piperazine 0-10 prion protein Homo sapiens 31-34 24502948-0 2014 Piperazine derivatives inhibit PrP/PrP(res) propagation in vitro and in vivo. Piperazine 0-10 prion protein Homo sapiens 35-38 24411201-4 2014 These structure-activity relationships are consistent with an X-ray structure of a representative compound bound in the AKR1C3 active site, which showed H-bonding between the carbonyl oxygen of the drug and Tyr55 and His117 in the "oxyanion hole" of the enzyme, with the piperazine bridging unit providing the correct twist to allow the terminal benzene ring to occupy the lipophilic pocket and align with Phe311. Piperazine 271-281 aldo-keto reductase family 1 member C3 Homo sapiens 120-126 24365161-1 2014 In this letter, we describe a series of 4-substituted piperidine and piperazine compounds based on tetrahydroquinoline 1, a compound that shows balanced, low nanomolar binding affinity for the mu opioid receptor (MOR) and the delta opioid receptor (DOR). Piperazine 69-79 opioid receptor mu 1 Homo sapiens 213-216 25335388-1 2014 We have studied the influence of new N,N"-substituted piperazines with variable nature of the linker between piperazine and aromatic cycles (carbonyl group in VR-0411 versus sulfonyl group in VR-0511) on thrombin-induced platelet aggregation, cytoplasmic Ca2+ mobilization in platelets, and P-selectin exposure on the platelet plasma membrane. Piperazine 54-64 coagulation factor II, thrombin Homo sapiens 204-212 23308267-0 2013 Design, synthesis and biological evaluation of novel piperazine derivatives as CCR5 antagonists. Piperazine 53-63 C-C motif chemokine receptor 5 Homo sapiens 79-83 23707730-8 2013 Moreover, the slo-1 mutant strain (completely emodepside resistant) also showed hypersusceptibility to piperazine. Piperazine 103-113 BK channel;Calcium-activated potassium channel slo-1 Caenorhabditis elegans 14-19 23707730-9 2013 Interestingly, neither the GABAA-R unc-49 mutants nor the AChR mutants showed decreased susceptibility against piperazine, although there were some studies that indicated an involvement of GABAA-R or AChR in the piperazine mode of action. Piperazine 212-222 Betaine receptor acr-23 Caenorhabditis elegans 200-204 24591157-0 2013 Design, synthesis, biological evaluation, and molecular modeling of coumarin-piperazine derivatives as acetylcholinesterase inhibitors. Piperazine 77-87 acetylcholinesterase (Cartwright blood group) Homo sapiens 103-123 24591157-4 2013 Docking experiments of the designed coumarin-piperazine derivatives were carried out in order to compare the theoretical and experimental binding affinities toward hAChE, to delineate the inhibitory mechanism. Piperazine 45-55 acetylcholinesterase (Cartwright blood group) Homo sapiens 164-169 24093059-9 2013 Our studies suggest that this piperazine derivative effectively (GI50 = 0.06-0.16 muM) inhibits cancer cell proliferation and induces caspase-dependent apoptosis via inhibiting multiple cancer signaling pathways including the PI3K/AKT, the Src family kinases and the BCR-ABL pathways. Piperazine 30-40 latexin Homo sapiens 82-85 24093059-9 2013 Our studies suggest that this piperazine derivative effectively (GI50 = 0.06-0.16 muM) inhibits cancer cell proliferation and induces caspase-dependent apoptosis via inhibiting multiple cancer signaling pathways including the PI3K/AKT, the Src family kinases and the BCR-ABL pathways. Piperazine 30-40 AKT serine/threonine kinase 1 Homo sapiens 231-234 24093059-9 2013 Our studies suggest that this piperazine derivative effectively (GI50 = 0.06-0.16 muM) inhibits cancer cell proliferation and induces caspase-dependent apoptosis via inhibiting multiple cancer signaling pathways including the PI3K/AKT, the Src family kinases and the BCR-ABL pathways. Piperazine 30-40 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 267-274 23748247-4 2013 We described an approach that combines molecular docking, molecular dynamics, MM-PBSA calculations and conformational analysis to rationally predict piperazine derivatives binding mode with HIV-1 gp120. Piperazine 149-159 Envelope surface glycoprotein gp160, precursor Human immunodeficiency virus 1 196-201 23923631-0 2013 Piperazine modification in 2,4,6-triaminopyrimidine derivatives as histamine H4 receptor ligands. Piperazine 0-10 histamine receptor H4 Homo sapiens 67-88 23266181-2 2013 Based on a piperazine alkyl derivative that induced apoptosis via up-regulation of RhoB, we synthesized novel aliphatic amido/sulfonamido-quaternary ammonium salts and evaluated their biological activities using an in vitro growth inhibition assay and RhoB promoter assay in human cancer cells. Piperazine 11-21 ras homolog family member B Homo sapiens 83-87 23521796-0 2013 Piperazine and piperidine triazole ureas as ultrapotent and highly selective inhibitors of monoacylglycerol lipase. Piperazine 0-10 monoglyceride lipase Homo sapiens 91-114 23521796-6 2013 Here, we have characterized piperazine and piperidine triazole ureas that combine the high potency attributable to the triazole leaving group together with the bulky aromatic benzodioxolyl moiety required for selectivity, culminating in compound JJKK-048 that potently (IC50 < 0.4 nM) inhibited human and rodent MAGL. Piperazine 28-38 monoglyceride lipase Homo sapiens 315-319 23039850-3 2013 Compounds 8 (IC(50) = 0.32 muM), 9 (IC(50) = 0.29 muM), and 12 (IC(50) = 0.25 muM) showed excellent dipeptidyl peptidase IV inhibition having heterocyclic substituted piperazine with acetamide linker resulted as most potent dipeptidyl peptidase IV inhibitors among all the compounds screened. Piperazine 167-177 dipeptidylpeptidase 4 Rattus norvegicus 100-123 24288651-0 2013 Virtual screening and biological evaluation of piperazine derivatives as human acetylcholinesterase inhibitors. Piperazine 47-57 acetylcholinesterase (Cartwright blood group) Homo sapiens 79-99 24288651-1 2013 The piperazine derivatives have been shown to inhibit human acetylcholinesterase. Piperazine 4-14 acetylcholinesterase (Cartwright blood group) Homo sapiens 60-80 22759791-3 2012 Using immunocytochemistry and NFkappaB-dependent secretory alkaline phosphatase (SEAP) analyses, bombesin induced NFkappaB activation in BMC-2 and RAW-blue macrophage cells, which was inhibited by MyD88 homodimerization inhibitor, Tamiflu, galardin, piperazine and anti-MMP-9 antibody. Piperazine 250-260 nuclear factor of kappa light polypeptide gene enhancer in B cells 1, p105 Mus musculus 114-122 22759791-3 2012 Using immunocytochemistry and NFkappaB-dependent secretory alkaline phosphatase (SEAP) analyses, bombesin induced NFkappaB activation in BMC-2 and RAW-blue macrophage cells, which was inhibited by MyD88 homodimerization inhibitor, Tamiflu, galardin, piperazine and anti-MMP-9 antibody. Piperazine 250-260 myeloid differentiation primary response gene 88 Mus musculus 197-202 22018919-5 2011 Biological evaluation of virtual hits led to the discovery of a novel FXR agonist with a piperazine scaffold (compound 19) that shows comparable activity as the endogenous FXR agonist chenodeoxycholic acid (CDCA, compound 2). Piperazine 89-99 nuclear receptor subfamily 1 group H member 4 Homo sapiens 70-73 22850208-2 2012 Several series of beta-amino amide containing piperazine derivatives have been prepared and evaluated as a inhibitor of DPP4. Piperazine 46-56 dipeptidyl peptidase 4 Homo sapiens 120-124 22412560-4 2012 These are sustained by O-H N(piperazine) hydrogen bonds, and are connected into the three-dimensional crystal structure by C-H S and C-H O inter-actions. Piperazine 29-39 lysosomal trafficking regulator Homo sapiens 123-136 22220821-9 2012 Through the screening of various spacer structures, piperazine was found to be optimal for FKBP12 labeling in terms of labeling efficiency and site specificity. Piperazine 52-62 FKBP prolyl isomerase 1A Homo sapiens 91-97 22220821-10 2012 Using a piperazine-based LDT reagent containing a photoreactive probe, we successfully demonstrated the labeling and UV-induced covalent cross-linking of FKBP12 and its interacting proteins in vitro and in living cells. Piperazine 8-18 FKBP prolyl isomerase 1A Homo sapiens 154-160 21880486-1 2011 Two novel series of 5-nitro-2-phenoxybenzoic acid derivatives are designed as potent PAI-1 inhibitors using hybridization and conformational restriction strategy in the tiplaxtinin and piperazine chemo types. Piperazine 185-195 serpin family E member 1 Homo sapiens 85-90 21957888-0 2011 The 5-HT(1A) agonism potential of substituted piperazine-ethyl-amide derivatives is conserved in the hexyl homologues: molecular modeling and pharmacological evaluation. Piperazine 46-56 5-hydroxytryptamine receptor 1A Rattus norvegicus 4-11 21711053-4 2011 The obtained results, together with earlier work from our group, clearly narrow down the most probable DPP8-selectivity imparting modification points in DPP8/9 inhibitors to parts of space that are topologically equivalent to the piperazine ring system in 7. Piperazine 230-240 dipeptidyl peptidase 8 Homo sapiens 103-107 21822520-1 2011 The solvothermal reaction of In(III) and 1,2,4,5-benzeneteracarboxylic acid with the presence of piperazine leads to the generation of a novel 3D chiral porous coordination polymer with PtS topological net. Piperazine 97-107 6-pyruvoyltetrahydropterin synthase Homo sapiens 186-189 21621413-1 2011 Starting from small molecule mTOR inhibitor Torin1, replacement of the piperazine ring with a phenyl ring resulted in a new series of mTOR inhibitors (as exemplified by 10) that showed superior potency and selectivity for mTOR, along with significantly improved mouse liver microsome stability and a longer in vivo half-life. Piperazine 71-81 mechanistic target of rapamycin kinase Mus musculus 134-138 21621413-1 2011 Starting from small molecule mTOR inhibitor Torin1, replacement of the piperazine ring with a phenyl ring resulted in a new series of mTOR inhibitors (as exemplified by 10) that showed superior potency and selectivity for mTOR, along with significantly improved mouse liver microsome stability and a longer in vivo half-life. Piperazine 71-81 mechanistic target of rapamycin kinase Mus musculus 134-138 19967721-4 2010 Various chemical classes of small molecule CCR3 antagonists have been described so far, including (bi)piperidine and piperazine derivatives, N-arylalkylpiperidine urea derivatives and (N-ureidoalkyl)benzylpiperidines, phenylalanine derivatives, morpholinyl derivatives, pyrrolidinohydroquinazolines, arylsulfonamides, amino-alkyl amides, imidazole- and pyrimidine-based antagonists, and bicyclic diamines. Piperazine 117-127 C-C motif chemokine receptor 3 Homo sapiens 43-47 21557566-1 2011 The reaction of VOSO(4) with 2-carboxyethylphosphonic acid (H(2)-CEP) in presence of piperazine (PIP) produces a 3D inorganic-organic hybrid framework, {(H(2)PIP)(0.5)[VO(CEP)] H(2)O} (1) with bidirectional channels occupied by the H(2)PIP cations and H(2)O molecules. Piperazine 85-95 prolactin induced protein Homo sapiens 97-100 21557566-1 2011 The reaction of VOSO(4) with 2-carboxyethylphosphonic acid (H(2)-CEP) in presence of piperazine (PIP) produces a 3D inorganic-organic hybrid framework, {(H(2)PIP)(0.5)[VO(CEP)] H(2)O} (1) with bidirectional channels occupied by the H(2)PIP cations and H(2)O molecules. Piperazine 85-95 prolactin induced protein Homo sapiens 158-161 21557566-1 2011 The reaction of VOSO(4) with 2-carboxyethylphosphonic acid (H(2)-CEP) in presence of piperazine (PIP) produces a 3D inorganic-organic hybrid framework, {(H(2)PIP)(0.5)[VO(CEP)] H(2)O} (1) with bidirectional channels occupied by the H(2)PIP cations and H(2)O molecules. Piperazine 85-95 prolactin induced protein Homo sapiens 158-161 25961263-6 2011 In the present study, we report that the dual inhibitory effect exerted by sildenafil on both XO and PDE-5 is a consequence of a structural modification induced by O2 -, also consisting of the release of a piperazine group that could in turn inhibit the XO enzyme. Piperazine 206-216 phosphodiesterase 5A Homo sapiens 101-106 21465559-4 2011 The piperazine group of BMS-488 prevents the bridging sheet formation of gp120 induced by the CD4 binding mainly through blocking the rotation of the Trp112 located on the alpha1 helix of gp120. Piperazine 4-14 inter-alpha-trypsin inhibitor heavy chain 4 Homo sapiens 73-78 21465559-4 2011 The piperazine group of BMS-488 prevents the bridging sheet formation of gp120 induced by the CD4 binding mainly through blocking the rotation of the Trp112 located on the alpha1 helix of gp120. Piperazine 4-14 CD4 molecule Homo sapiens 94-97 21465559-4 2011 The piperazine group of BMS-488 prevents the bridging sheet formation of gp120 induced by the CD4 binding mainly through blocking the rotation of the Trp112 located on the alpha1 helix of gp120. Piperazine 4-14 inter-alpha-trypsin inhibitor heavy chain 4 Homo sapiens 188-193 21290451-3 2011 The effect of piperazine derivatives on the signals of tryptic digests of alpha-transferrin and bovine serum albumin (BSA) was investigated, and it was found that peptides derivatized by 2-PP and 2-PMP exhibited obviously improved ionization efficiency. Piperazine 14-24 albumin Rattus norvegicus 103-116 20414792-2 2011 As a first step in the 3D-QSAR modeling of the dopamine transporter (DAT)/serotonin transporter (SERT) selectivity of these compounds, we carried out conformational analyses of two analogs of 1: a piperazine (2) and a related piperidine (3). Piperazine 197-207 solute carrier family 6 member 3 Homo sapiens 47-67 20414792-2 2011 As a first step in the 3D-QSAR modeling of the dopamine transporter (DAT)/serotonin transporter (SERT) selectivity of these compounds, we carried out conformational analyses of two analogs of 1: a piperazine (2) and a related piperidine (3). Piperazine 197-207 solute carrier family 6 member 3 Homo sapiens 69-72 20414792-2 2011 As a first step in the 3D-QSAR modeling of the dopamine transporter (DAT)/serotonin transporter (SERT) selectivity of these compounds, we carried out conformational analyses of two analogs of 1: a piperazine (2) and a related piperidine (3). Piperazine 197-207 solute carrier family 6 member 4 Homo sapiens 97-101 21074434-0 2010 Design, synthesis, and structure-activity relationship study of bicyclic piperazine analogs of indole-3-carboxamides as novel cannabinoid CB1 receptor agonists. Piperazine 73-83 cannabinoid receptor 1 Homo sapiens 138-141 21074434-1 2010 Bicyclic piperazine derivatives were synthesized as conformationally constrained analogs of N-alkyl piperazines and were found to be potent CB1 receptor agonists. Piperazine 9-19 cannabinoid receptor 1 Homo sapiens 140-143 20947352-1 2010 Utilization of a tetrahydro-pyrimdoazepine core as a bioisosteric replacement for a piperazine-urea resulted in the discovery a novel series of potent antagonists of TRPV1. Piperazine 84-94 transient receptor potential cation channel subfamily V member 1 Homo sapiens 166-171 20538497-2 2010 Ligand-based pharmacophore models of N-Aryl and N-Heteroaryl piperazine alpha(1A)-antagonists were developed using two separate training sets. Piperazine 61-71 calcium voltage-gated channel subunit alpha1 A Homo sapiens 72-80 21711053-4 2011 The obtained results, together with earlier work from our group, clearly narrow down the most probable DPP8-selectivity imparting modification points in DPP8/9 inhibitors to parts of space that are topologically equivalent to the piperazine ring system in 7. Piperazine 230-240 dipeptidyl peptidase 8 Homo sapiens 153-157 21598199-4 2011 In this context, a QSAR study of hSERT inhibitory and H(3) antagonistic activity of piperazine and diazepane amide derivatives has been carried out using the combinatorial protocol in multiple linear regression (CP-MLR) with 0D- to 2D-Dragon descriptors. Piperazine 84-94 solute carrier family 6 member 4 Homo sapiens 33-38 21598199-5 2011 The derived QSAR models have provided a rational approach for the development of new piperazine and diazepane amide derivatives as hSERT inhibitors and H(3) antagonists. Piperazine 85-95 solute carrier family 6 member 4 Homo sapiens 131-136 21327226-2 2011 Co(12)(OH)(18)(ox)(3)(pip) [ox = oxalate, C(2)O(4)(2-); pip = piperazine, C(4)N(2)H(10)] (1), is essentially built from brucite-like layers with a one ninth depletion of the octahedral sites and a preservation of a trigonal crystallographic symmetry. Piperazine 62-72 prolactin induced protein Homo sapiens 22-25 20833551-3 2010 Among the compounds synthesized, urea derivative 11l having a piperazine moiety on the terminal benzene ring showed strong inhibitory activity against FGFR1 kinase as well as VEGFR2 kinase. Piperazine 62-72 fibroblast growth factor receptor 1 Homo sapiens 151-156 20833551-3 2010 Among the compounds synthesized, urea derivative 11l having a piperazine moiety on the terminal benzene ring showed strong inhibitory activity against FGFR1 kinase as well as VEGFR2 kinase. Piperazine 62-72 kinase insert domain receptor Homo sapiens 175-181 20833551-4 2010 A binding model of 11l complexed with VEGFR2 suggested that the piperazine moiety forms additional interactions with Ile1025 and His1026. Piperazine 64-74 kinase insert domain receptor Homo sapiens 38-44 21779428-8 2010 The increased potency observed for the second-generation "type II" inhibitors was observed to be due to an improved interaction with the ATP pocket of FLT3, specifically associated with introduction of a piperazine moiety and placement of an amino group in position 2 of the pyrimidine ring. Piperazine 204-214 fms related receptor tyrosine kinase 3 Homo sapiens 151-155 20371179-0 2010 Discovery of novel leukotriene A4 hydrolase inhibitors based on piperidine and piperazine scaffolds. Piperazine 79-89 leukotriene A4 hydrolase Homo sapiens 19-43 20347189-1 2010 By employing pharmacophore-based design and the privileged fragments reassembly, a series of piperidine-/tropane-/piperazine-bridged CCR5 antagonists were designed and synthesized via an efficient convergent synthesis strategy, with focus on the optimal choice of the basic center carrier structure. Piperazine 114-124 C-C motif chemokine receptor 5 Homo sapiens 133-137 20371179-1 2010 Novel piperidine and piperazine derivatives have been designed and tested as inhibitors of LTA(4) hydrolase (LTA(4)H). Piperazine 21-31 leukotriene A4 hydrolase Homo sapiens 91-107 20371179-1 2010 Novel piperidine and piperazine derivatives have been designed and tested as inhibitors of LTA(4) hydrolase (LTA(4)H). Piperazine 21-31 leukotriene A4 hydrolase Homo sapiens 109-116 20223662-2 2010 Structure-activity studies on 3-aminopyrrolidine incorporating heteroatomic carbocycle moieties led to piperidine compound 19, and piperazine compounds 42, 47 and 49 as highly potent hCCR2 antagonists. Piperazine 131-141 C-C motif chemokine receptor 2 Homo sapiens 183-188 20099888-2 2010 We have recently discovered that MAGL and FAAH are both inhibited by carbamates bearing an N-piperidine/piperazine group. Piperazine 104-114 monoglyceride lipase Mus musculus 33-37 20137933-1 2010 Piperazine-bisamide analogs were discovered as partial agonists of human growth hormone secretagogue receptor (GHSR) in a high throughput screen. Piperazine 0-10 growth hormone secretagogue receptor Homo sapiens 73-109 20137933-1 2010 Piperazine-bisamide analogs were discovered as partial agonists of human growth hormone secretagogue receptor (GHSR) in a high throughput screen. Piperazine 0-10 growth hormone secretagogue receptor Homo sapiens 111-115 20088516-2 2010 We used a known 5-HT(1B) antagonist template as our starting point and focused on replacing the piperazine moiety. Piperazine 96-106 5-hydroxytryptamine receptor 1B Homo sapiens 16-23 20078106-5 2010 Thus, we propose that D3.32 in TM 3 anchors the protonated piperazine ring, the benzimidazole ring expands parallel to EL 2 to hydrogen bond N6.55 in TM 6, and the aromatic ring is placed between TMs 3 and 5 in CH(2)-containing compounds and between TMs 3 and 6 in CO-containing compounds. Piperazine 59-69 tropomyosin 3 Homo sapiens 31-35 19926281-1 2010 Starting from a known piperazine-based SCD-1 inhibitor, we obtained more potent benzoylpiperidine analogs. Piperazine 22-32 stearoyl-CoA desaturase Rattus norvegicus 39-44 20217840-0 2010 Inhibitors of human histone deacetylase: synthesis and enzyme assay of hydroxamates with piperazine linker. Piperazine 89-99 histone deacetylase 9 Homo sapiens 20-39 20099888-5 2010 These scaffolds can be tuned for MAGL-selective or dual MAGL-FAAH inhibition by the attachment of an appropriately substituted bisarylcarbinol or aryloxybenzyl moiety, respectively, on the piperidine/piperazine ring. Piperazine 200-210 monoglyceride lipase Mus musculus 33-37 20099888-5 2010 These scaffolds can be tuned for MAGL-selective or dual MAGL-FAAH inhibition by the attachment of an appropriately substituted bisarylcarbinol or aryloxybenzyl moiety, respectively, on the piperidine/piperazine ring. Piperazine 200-210 monoglyceride lipase Mus musculus 56-60 20099888-5 2010 These scaffolds can be tuned for MAGL-selective or dual MAGL-FAAH inhibition by the attachment of an appropriately substituted bisarylcarbinol or aryloxybenzyl moiety, respectively, on the piperidine/piperazine ring. Piperazine 200-210 fatty acid amide hydrolase Mus musculus 61-65 20212915-8 2010 Proposition #5 The first 3 amino acid sequences of beta endorphin (l-try-gly-gly) and the active opioid dipeptide, l-tyr-pro, (as a result of a peptide turn and zwitterion bonding) form a virtual piperazine-like ring which is similar in size, shape and location to the heterocyclic rings of morphine, meperidine, and methadone. Piperazine 196-206 proopiomelanocortin Homo sapiens 51-65 20022748-3 2010 However, the replacement of the piperazine moiety by a 1,2,3,6-tetrahydropyridine ring in 4-arylpiperazine-ethyl carboxamide derivatives was recently shown to be highly favourable for 5-HT(1A) affinity. Piperazine 32-42 5-hydroxytryptamine receptor 1A Homo sapiens 184-191 20099888-2 2010 We have recently discovered that MAGL and FAAH are both inhibited by carbamates bearing an N-piperidine/piperazine group. Piperazine 104-114 fatty acid amide hydrolase Mus musculus 42-46 19589229-9 2009 CONCLUSIONS: Fluorophenylpiperazine, methoxyphenylpiperazine, chlorophenylpiperazine, methylbenzylpiperazine and methylenedioxybenzylpiperazine had significant inhibitory effects on CYP2D6, CYP1A2, CYP3A4, CYP2C19 and CYP2C9 isoenzymes but each piperazine had a different inhibitory profile. Piperazine 25-35 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 182-188 19664921-4 2009 The piperazine ring was shown to be a critical element of the HIV-1 attachment inhibiting pharmacophore, acting as a scaffold to deploy the indole glyoxamide and benzamide in a topographical relationship that complements the binding site on gp120. Piperazine 4-14 Envelope surface glycoprotein gp160, precursor Human immunodeficiency virus 1 241-246 19904008-1 2009 The aim of the present study was to estimate the inhibitory effect of perazine, a phenothiazine neuroleptic with piperazine structure in a side chain, on human CYP1A2 activity measured as a rate of caffeine 3-N- and 1-N-demethylation. Piperazine 113-123 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 160-166 19601612-1 2009 Bipyridazines were modified with heterocyclic amines such as piperazine to give symmetric quadrupolar (SPBP) and asymmetric dipolar (APBP) bipyridazine. Piperazine 61-71 transcription factor 20 Homo sapiens 103-107 19916484-0 2009 Al(OTf)(3)-mediated epoxide ring-opening reactions: toward piperazine-derived physiologically active products. Piperazine 59-69 POU class 5 homeobox 1 Homo sapiens 0-9 19916484-1 2009 Al(OTf)(3) is a good catalyst for the ring opening of epoxides, forming beta-amino alcohols bearing the piperazine motif. Piperazine 104-114 POU class 5 homeobox 1 Homo sapiens 0-9 19460190-4 2009 We report herein a novel piperazine derivative compound PMS1339 possesses multifunctional properties including anti-platelet-activating factor, AChE inhibition, Abeta aggregation inhibition and cognitive improvement. Piperazine 25-35 acetylcholinesterase Mus musculus 144-148 19589229-9 2009 CONCLUSIONS: Fluorophenylpiperazine, methoxyphenylpiperazine, chlorophenylpiperazine, methylbenzylpiperazine and methylenedioxybenzylpiperazine had significant inhibitory effects on CYP2D6, CYP1A2, CYP3A4, CYP2C19 and CYP2C9 isoenzymes but each piperazine had a different inhibitory profile. Piperazine 25-35 cytochrome P450 family 1 subfamily A member 2 Homo sapiens 190-196 19589229-9 2009 CONCLUSIONS: Fluorophenylpiperazine, methoxyphenylpiperazine, chlorophenylpiperazine, methylbenzylpiperazine and methylenedioxybenzylpiperazine had significant inhibitory effects on CYP2D6, CYP1A2, CYP3A4, CYP2C19 and CYP2C9 isoenzymes but each piperazine had a different inhibitory profile. Piperazine 25-35 cytochrome P450 family 3 subfamily A member 4 Homo sapiens 198-204 19589229-9 2009 CONCLUSIONS: Fluorophenylpiperazine, methoxyphenylpiperazine, chlorophenylpiperazine, methylbenzylpiperazine and methylenedioxybenzylpiperazine had significant inhibitory effects on CYP2D6, CYP1A2, CYP3A4, CYP2C19 and CYP2C9 isoenzymes but each piperazine had a different inhibitory profile. Piperazine 25-35 cytochrome P450 family 2 subfamily C member 19 Homo sapiens 206-213 19589229-9 2009 CONCLUSIONS: Fluorophenylpiperazine, methoxyphenylpiperazine, chlorophenylpiperazine, methylbenzylpiperazine and methylenedioxybenzylpiperazine had significant inhibitory effects on CYP2D6, CYP1A2, CYP3A4, CYP2C19 and CYP2C9 isoenzymes but each piperazine had a different inhibitory profile. Piperazine 25-35 cytochrome P450 family 2 subfamily C member 9 Homo sapiens 218-224 18630921-2 2008 The usefulness of this structural surrogate of piperazine is shown in arene amination reactions yielding a variety of N-Boc- N"-aryl-2,6-diazaspiro[3.3]heptanes. Piperazine 47-57 BOC cell adhesion associated, oncogene regulated Homo sapiens 120-123 18811147-3 2008 Piperazine or 2,6-dimethylpiperazine reacts with carbon disulfide to give the zwitterionic dithiocarbamate salts H2NC4H6(R2-3,5)NCS2 (R = H; R = Me), which form the complexes [Ru(S2CNC4H6(R2-3,5)NH2)(dppm)2](2+) on reaction with cis-[RuCl2(dppm)2]. Piperazine 0-10 cytosolic thiouridylase subunit 2 Homo sapiens 128-132 19143029-0 2009 Piperazine-designed alpha 1A/alpha 1D-adrenoceptor blocker KMUP-1 and doxazosin provide down-regulation of androgen receptor and PSA in prostatic LNCaP cells growth and specifically in xenografts. Piperazine 0-10 androgen receptor Homo sapiens 107-124 19143029-0 2009 Piperazine-designed alpha 1A/alpha 1D-adrenoceptor blocker KMUP-1 and doxazosin provide down-regulation of androgen receptor and PSA in prostatic LNCaP cells growth and specifically in xenografts. Piperazine 0-10 kallikrein related peptidase 3 Homo sapiens 129-132 18720282-0 2008 Strategies to prevent N-acetyltransferase-mediated metabolism in a series of piperazine-containing pyrazalopyrimidine compounds. Piperazine 77-87 N-acetyltransferase 1 Rattus norvegicus 22-41 18720282-13 2008 Further experiments showed that it was possible to make small structural changes to the piperazine group that retained potency but prevented metabolism by NAT. Piperazine 88-98 N-acetyltransferase 1 Rattus norvegicus 155-158 18396900-5 2008 To minimize the interactions between activated MMPs and the dye of the conjugate 6, a PEGylated piperazine derivative was used as a spacer and an azide as a protected amino function. Piperazine 96-106 matrix metallopeptidase 2 Homo sapiens 47-51 18557608-2 2008 These efforts led to the discovery of a piperazine-containing analogue, 17g (WY-46824), that exhibited potent norepinephrine reuptake inhibition, excellent selectivity over the serotonin transporter, but no selectivity over the dopamine transporter. Piperazine 40-50 solute carrier family 6 member 3 Homo sapiens 228-248 18243711-0 2008 Design, synthesis and biological evaluation of piperazine analogues as CB1 cannabinoid receptor ligands. Piperazine 47-57 cannabinoid receptor 1 Homo sapiens 71-74 18078749-1 2008 Analogues of the P2X(7) receptor antagonist KN-62, modified at the piperazine and arylsulfonyl groups, were synthesized and assayed at the human P2X(7) receptor for inhibition of BzATP-induced effects, that is, uptake of a fluorescent dye (ethidium bromide) in stably transfected HEK293 cells and IL-1beta release in differentiated THP-1 cells. Piperazine 67-77 purinergic receptor P2X 7 Homo sapiens 17-32 17855089-2 2007 The amino(methyl) pyrrolidine scaffolds were designed based on the proposed bioisosterism to the piperazine core in known FXa inhibitors. Piperazine 97-107 coagulation factor X Homo sapiens 122-125 17763374-5 2007 Docking analysis indicated that the binding to D(2) and 5-HT(1A) receptors is based on (i) interaction between protonated N1 of the piperazine ring and various aspartate residues, (ii) hydrogen bonds between various moieties of the ligand and the residues of threonine, serine, histidine or tryptophane, and (iii) edge-to-face interactions of the aromatic ring of the arylpiperazine moiety with phenylalanine or tyrosine residues. Piperazine 132-142 5-hydroxytryptamine receptor 1A Homo sapiens 56-63 18019544-4 2007 Thus, a SAR study of our synthesized piperazinopiperidine-based CCR5 antagonists was conducted with respect to the structure and configuration of the substituent on the piperazine ring. Piperazine 169-179 C-C motif chemokine receptor 5 Homo sapiens 64-68 18019544-6 2007 By using the forward-synthesis approach, the best compound in the chiral piperazine-based CCR5 antagonist series, Sch-D (Vicriviroc), was conveniently synthesized in an excellent yield. Piperazine 73-83 C-C motif chemokine receptor 5 Homo sapiens 90-94 17555959-1 2007 This paper describes the synthesis of orally available potent fXa inhibitors 2 and 3 by modification of the piperazine part of lead compound 1. Piperazine 108-118 coagulation factor X Homo sapiens 62-65 16893650-1 2006 Part 13: synthesis and biological evaluation of piperazine derivatives with dual anti-PAF and anti-HIV-1 or pure antiretroviral activity. Piperazine 48-58 PCNA clamp associated factor Homo sapiens 86-89 16821787-5 2006 Variable temperature NMR and modeling studies are consistent with the obtained biological data, since these studies confirmed that introduction at the N(4)-position of the piperazine ring allows productive interactions within the BACE-1 active site, which appear to be determinative for high BACE-1 inhibitory activity. Piperazine 172-182 beta-secretase 1 Homo sapiens 230-236 17034141-5 2006 The 3-position on the piperazine ring was also found to play an appreciable role, as substitutions in that position exerted a significant and stereospecific beneficial effect on the alpha(2C)-adrenoceptor affinity and potency. Piperazine 22-32 adrenoceptor alpha 2C Homo sapiens 182-204 16908170-1 2006 Part 14: synthesis and biological evaluation of piperazine derivatives with dual anti-PAF and anti-HIV-1 activity. Piperazine 48-58 TCDD inducible poly(ADP-ribose) polymerase Homo sapiens 0-7 16870426-1 2006 Bioisosteric replacement of piperazine with an aryl ring in lead VR1 antagonist 1 led to the biarylamide series. Piperazine 28-38 transient receptor potential cation channel subfamily V member 1 Homo sapiens 65-68 16821787-5 2006 Variable temperature NMR and modeling studies are consistent with the obtained biological data, since these studies confirmed that introduction at the N(4)-position of the piperazine ring allows productive interactions within the BACE-1 active site, which appear to be determinative for high BACE-1 inhibitory activity. Piperazine 172-182 beta-secretase 1 Homo sapiens 292-298 15771443-1 2005 Piperazine derivatives of 2-furanyl[1,2,4]triazolo[1,5-a][1,3,5]triazine have recently been demonstrated to be potent and selective adenosine A(2a) receptor antagonists with oral activity in rodent models of Parkinson"s disease. Piperazine 0-10 adenosine A2a receptor Mus musculus 132-156 16787355-4 2006 In the present study we report that PARP-1 inhibitor 3-aminobenzamide (3-AB) increases the cytotoxic activity of the platinum compounds cisplatin, trans-[PtCl(2)(4-picoline)(piperazine)] and transplatin against CH1cisR cisplatin-resistant ovarian tumor cells. Piperazine 174-184 poly(ADP-ribose) polymerase 1 Homo sapiens 36-42 18007345-2 2005 The Co(III)ion is six-coordinated with octahedral geometry, the pyridine rings are planar and the piperazine rings assume chair conformations. Piperazine 98-108 mitochondrially encoded cytochrome c oxidase III Homo sapiens 4-11 16153839-1 2005 An SAR study around the mixed 5-HT1ABD receptor antagonist SB-272183 found that introduction of cis-2,6-dimethyl substitution onto the piperazine ring was a key structural change, which imparted a combination of both excellent selectivity over the 5-HT1A and 5-HT1D receptors and low intrinsic activity. Piperazine 135-145 5-hydroxytryptamine receptor 1A Homo sapiens 30-36 15848206-1 2005 The crystal structure of Acetylcholine Binding Protein (AChBP), homolog of the ligand binding domain of nAChR, has been used as model for computational investigations on the ligand-receptor interactions of derivatives of 6-chloropyridazine substituted at C3 with 3,8-diazabicyclo[3.2.1]octane, 2,5-diazabicyclo[2.2.1]heptane and with piperazine and homopiperazine, substituted or not at N4. Piperazine 334-344 cholinergic receptor nicotinic alpha 4 subunit Homo sapiens 104-109 15745810-1 2005 The biological activity for a set of melanocortin-4 receptor (MC4R) agonists containing a piperazine core with an ortho-substituted aryl sulfonamide is described. Piperazine 90-100 melanocortin 4 receptor Mus musculus 37-60 15745810-1 2005 The biological activity for a set of melanocortin-4 receptor (MC4R) agonists containing a piperazine core with an ortho-substituted aryl sulfonamide is described. Piperazine 90-100 melanocortin 4 receptor Mus musculus 62-66 15713417-0 2005 Benzothiophenes containing a piperazine side chain as selective ligands for the estrogen receptor alpha and their bioactivities in vivo. Piperazine 29-39 estrogen receptor 1 Homo sapiens 80-103 15713417-2 2005 These compounds bearing piperazine side chains were identified to be high-affinity ligands with high selectivity for ER alpha subtype. Piperazine 24-34 estrogen receptor 1 Homo sapiens 117-125 15694651-1 2005 New benzoindolinothiazepines containing a piperazine moiety are described as potent antiproliferative agents against PC3 human prostatic cell lines. Piperazine 42-52 chromobox 8 Homo sapiens 117-120 15581370-4 2004 Interestingly, previous studies showed that piperazine, an inexpensive and safe anthelmintic, both inhibits IRK1 channels and is antiarrhythmic in some animal preparations. Piperazine 44-54 potassium inwardly-rectifying channel, subfamily J, member 2 Mus musculus 108-112 15581370-5 2004 This potential pharmacological benefit motivated us to further characterize the energetic, kinetic, and molecular properties of IRK1 inhibition by piperazine. Piperazine 147-157 potassium inwardly-rectifying channel, subfamily J, member 2 Mus musculus 128-132 15340914-7 2004 The Tyr side-chains of L32, L92, H100, and H100A form nonpolar contacts with the HEPES ethylene and piperazine groups. Piperazine 100-110 ribosomal protein L32 Homo sapiens 23-26 15497993-4 2004 Reaction of 6 with piperazine proceeded irreversibly to provide an isomeric mixture of piperazine products, with the syn:anti product ratio increased by solvent effects. Piperazine 19-29 synemin Homo sapiens 117-120 15497993-4 2004 Reaction of 6 with piperazine proceeded irreversibly to provide an isomeric mixture of piperazine products, with the syn:anti product ratio increased by solvent effects. Piperazine 87-97 synemin Homo sapiens 117-120 15203141-0 2004 Facile synthesis of 4-substituted-4-aminopiperidine derivatives, the key building block of piperazine-based CCR5 antagonists. Piperazine 91-101 C-C motif chemokine receptor 5 Homo sapiens 108-112 15294001-0 2004 Piperazine derivatives of [1,2,4]triazolo[1,5-a][1,3,5]triazine as potent and selective adenosine A2a receptor antagonists. Piperazine 0-10 adenosine A2a receptor Rattus norvegicus 88-110 12482418-2 2003 Most of the new compounds showed high affinity for the three types of receptors alpha(1A), D(2) and 5-HT(2A) which depends, fundamentally, on the substitution of the N(4) of the piperazine ring. Piperazine 178-188 calcium voltage-gated channel subunit alpha1 A Homo sapiens 80-88 15228152-8 2004 In summary, polymorphically expressed CYP2D6 was the major enzyme catalyzing the major metabolic steps of the studied piperazine- and pyrrolidinophenone-derived designer drugs. Piperazine 118-128 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 38-44 14741285-0 2004 Synthesis and biological evaluation of piperazine-based derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1). Piperazine 39-49 serpin family E member 1 Homo sapiens 85-118 14741285-0 2004 Synthesis and biological evaluation of piperazine-based derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1). Piperazine 39-49 serpin family E member 1 Homo sapiens 120-125 14599021-6 2003 The effect of 7-OH deprotonation yields a high frequency shift of 7-8 ppm on the C-7 carbon atom of the piperazine complex whereas it is as large as 12 ppm in the morpholine complex in the solid. Piperazine 104-114 complement C7 Homo sapiens 81-84 14521412-0 2003 Generation of predictive pharmacophore models for CCR5 antagonists: study with piperidine- and piperazine-based compounds as a new class of HIV-1 entry inhibitors. Piperazine 95-105 C-C motif chemokine receptor 5 Homo sapiens 50-54 14521412-1 2003 Predictive pharmacophore models were developed for a large series of piperidine- and piperazine-based CCR5 antagonists as anti-HIV-1 agents reported by Schering-Plough Research Institute in recent years. Piperazine 85-95 C-C motif chemokine receptor 5 Homo sapiens 102-106 15158798-6 2004 In this series the p-methoxybenzyl substituted piperazine 3d reveals the highest sigma1-receptor affinity (Ki=12.4 nM) with selectivity toward sigma2-, NMDA-, kappa-opioid, and mu-opioid receptors. Piperazine 47-57 sigma non-opioid intracellular receptor 1 Rattus norvegicus 81-96 15115380-0 2004 Piperazine-based CCR5 antagonists as HIV-1 inhibitors. Piperazine 0-10 C-C motif chemokine receptor 5 Homo sapiens 17-21 15056479-0 2004 The metabolism of the piperazine-type phenothiazine neuroleptic perazine by the human cytochrome P-450 isoenzymes. Piperazine 22-32 cytochrome P450 family 4 subfamily F member 3 Homo sapiens 86-102 14613328-7 2003 Relative binding affinity of the tethers bound to the targeting group for human androgen receptor were measured using a (3)H-Mibolerone competition assay and varied from 18% of nilutamide binding for the butynediol-based linear region to less than 1% for one of the piperazine derivatives. Piperazine 266-276 androgen receptor Homo sapiens 80-97 12951101-0 2003 Synthesis and biological activity of piperazine-based dual MMP-13 and TNF-alpha converting enzyme inhibitors. Piperazine 37-47 matrix metallopeptidase 13 Homo sapiens 59-65 12951101-0 2003 Synthesis and biological activity of piperazine-based dual MMP-13 and TNF-alpha converting enzyme inhibitors. Piperazine 37-47 tumor necrosis factor Homo sapiens 70-79 12593649-3 2003 The scaffold comprising the sulfonyl keto piperazine moiety might play a pivotal role in the orientation of substituents, since there is a strong hydrogen bond between Gly219 of fXa and the carbonyl oxygen of the piperazine. Piperazine 42-52 coagulation factor X Homo sapiens 178-181 12127516-0 2002 Pyrrolylquinoxalinediones carrying a piperazine residue represent highly potent and selective ligands to the homomeric kainate receptor GluR5. Piperazine 37-47 glutamate ionotropic receptor kainate type subunit 1 Homo sapiens 136-141 12372512-0 2002 Indoline and piperazine containing derivatives as a novel class of mixed D(2)/D(4) receptor antagonists. Piperazine 13-23 dopamine receptor D4 Homo sapiens 78-91 11856033-5 2002 Piperazine reacts with 4 in the presence of DCC and BtOH to form a bisfullerene derivative in which two sebacoyl chains and the piperazine act as the bridge between two molecules of 1. Piperazine 0-10 DCC netrin 1 receptor Homo sapiens 44-47 11882001-4 2002 The two-carbon spacer between the hydroxyl group and the piperazine ring was essential for enantioselectivity, and the length of the alkyl chain between the phenyl group and the piperazine ring influenced binding affinity and selectivity for the DAT and SERT. Piperazine 57-67 solute carrier family 6 member 3 Macaca mulatta 246-249 11882001-4 2002 The two-carbon spacer between the hydroxyl group and the piperazine ring was essential for enantioselectivity, and the length of the alkyl chain between the phenyl group and the piperazine ring influenced binding affinity and selectivity for the DAT and SERT. Piperazine 178-188 solute carrier family 6 member 3 Macaca mulatta 246-249 11856033-5 2002 Piperazine reacts with 4 in the presence of DCC and BtOH to form a bisfullerene derivative in which two sebacoyl chains and the piperazine act as the bridge between two molecules of 1. Piperazine 128-138 DCC netrin 1 receptor Homo sapiens 44-47 11585438-0 2001 Piperazine-based CCR5 antagonists as HIV-1 inhibitors. Piperazine 0-10 C-C motif chemokine receptor 5 Homo sapiens 17-21 11848227-1 2002 New muq-opioid receptor (MOR) agonists containing 4-hydroxypiperidine, piperidine and piperazine moieties were synthesized and evaluated to find a peripheral opioid analgesic. Piperazine 86-96 opioid receptor mu 1 Homo sapiens 4-23 11848227-1 2002 New muq-opioid receptor (MOR) agonists containing 4-hydroxypiperidine, piperidine and piperazine moieties were synthesized and evaluated to find a peripheral opioid analgesic. Piperazine 86-96 opioid receptor mu 1 Homo sapiens 25-28 11689071-0 2001 Three-dimensional quantitative structure-activity relationship (3D-QSAR) models for a novel class of piperazine-based stromelysin-1 (MMP-3) inhibitors: applying a "divide and conquer" strategy. Piperazine 101-111 matrix metallopeptidase 3 Homo sapiens 118-131 11689071-0 2001 Three-dimensional quantitative structure-activity relationship (3D-QSAR) models for a novel class of piperazine-based stromelysin-1 (MMP-3) inhibitors: applying a "divide and conquer" strategy. Piperazine 101-111 matrix metallopeptidase 3 Homo sapiens 133-138 11585438-4 2001 Further optimization for pharmacokinetic properties afforded Sch-350634 (1), a prototypical piperazine-based CCR5 antagonist, which is a potent inhibitor of HIV-1 entry and replication in PBMCs. Piperazine 92-102 C-C motif chemokine receptor 5 Homo sapiens 109-113 11605661-0 2001 New mu-opioid receptor agonists with piperazine moiety. Piperazine 37-47 opioid receptor mu 1 Homo sapiens 4-22 11605661-1 2001 New mu-opioid receptor (MOR) agonists containing piperazine and homopiperazine moieties in the structures were synthesized and their affinities to and agonist potencies on MOR were evaluated. Piperazine 49-59 opioid receptor mu 1 Homo sapiens 4-22 11605661-1 2001 New mu-opioid receptor (MOR) agonists containing piperazine and homopiperazine moieties in the structures were synthesized and their affinities to and agonist potencies on MOR were evaluated. Piperazine 49-59 opioid receptor mu 1 Homo sapiens 24-27 11738488-5 2001 In addition structure-activity relationships allow new hypothesis on interaction of these piperazine derivatives with the catalytic site of PLA(2)s. Piperazine 90-100 phospholipase A2 group IIA Homo sapiens 140-147 10669564-4 2000 X-ray crystallography data obtained for MMP-3 cocrystallized with 20 gave detailed information on key binding interactions defining an overall scaffold geometry for piperazine-based MMP inhibitors. Piperazine 165-175 matrix metallopeptidase 3 Homo sapiens 40-45 11672885-6 2001 Other predicted COX-2 selective compounds included are N--H indole-2-carboxylic acid diethyl 30 and piperazine 34 esters. Piperazine 100-110 mitochondrially encoded cytochrome c oxidase II Homo sapiens 16-21 11514156-0 2001 Piperazine-based CCR5 antagonists as HIV-1 inhibitors. Piperazine 0-10 C-C motif chemokine receptor 5 Homo sapiens 17-21 10841793-5 2000 Piperazine derivatives bearing a "cache-oreilles" (ear-muff) electronic distribution are able to inhibit in vitro PAF effects and, thus, could be used in pathologies where this mediator is involved. Piperazine 0-10 PCNA clamp associated factor Homo sapiens 114-117 11229767-3 2001 A smaller N-substituent in the piperazine ring was required for inhibition of TNF-alpha production. Piperazine 31-41 tumor necrosis factor Homo sapiens 78-87 10941138-0 2000 Piperazine analog of vesamicol: in vitro and in vivo characterization for vesicular acetylcholine transporter. Piperazine 0-10 solute carrier family 18 member A3 Rattus norvegicus 74-109 10941138-3 2000 We found that the piperazine analog of iodobenzovesamicol, trans-5-iodo-2-hydroxy-3-[4-phenylpiperazinyl] tetralin (DRC140), had high affinity for VAChT in rat brain. Piperazine 18-28 solute carrier family 18 member A3 Rattus norvegicus 147-152 10858318-15 2000 Consequently, and in contrast to morpholine, N-nitrosation of piperazine (2 mM) by both (*)NO/O(2) (PAPA NONOate, 0.5 mM) and the (*)NO/O(2)(-)(*)-releasing compound SIN-1 (1 mM) was inhibited by about 66% in the presence of 200 mM HCO(3)(-). Piperazine 62-72 pappalysin 1 Homo sapiens 100-104 10858318-15 2000 Consequently, and in contrast to morpholine, N-nitrosation of piperazine (2 mM) by both (*)NO/O(2) (PAPA NONOate, 0.5 mM) and the (*)NO/O(2)(-)(*)-releasing compound SIN-1 (1 mM) was inhibited by about 66% in the presence of 200 mM HCO(3)(-). Piperazine 62-72 MAPK associated protein 1 Homo sapiens 166-171 10881999-4 2000 The results pointed out the critical role of the group linked in the N-1 position of the piperazine in terms of 5-HT1A binding affinity. Piperazine 89-99 5-hydroxytryptamine receptor 1A Homo sapiens 112-118 9781839-8 1998 In conclusion, the C-7 substituted piperazine moiety of the molecules of already-known fluoroquinolone antibiotics may be responsible for the ability to increase cutaneous vascular permeability, whereas T-3762 is practically inactive because the free amino nitrogen of the 1-aminocyclopropyl group is conformationally present at a shorter distance from the carbon atom at position 7 of the ring nucleus. Piperazine 35-45 complement C7 Canis lupus familiaris 19-22 10649982-1 2000 N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide (1), a high-affinity and selective dopamine D(4) receptor ligand, was chosen as a lead, and structural modifications were done on its amide bond and on its alkyl chain linking the benzamide moiety to the piperazine ring and by preparing some semirigid analogues. Piperazine 24-33 dopamine receptor D4 Homo sapiens 100-122 10082215-1 1999 Previous studies have indicated that part of the binding of [3H] [1-[2-(diphenylmethoxy)ethyl]-4-(3-phenylpropyl) piperazine dihydrochloride] ([3H]GBR 12935) to human platelets is to a piperazine acceptor site, which might be associated with cytochrome P-450IID6 (CYP4502D6, debrisoquine-4-hydroxylase). Piperazine 114-124 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 275-301 10560726-2 1999 In the SAR study, the aryl substituents on the piperazine nitrogen were found to play an important role for the anti-HIV-1 activity. Piperazine 47-57 sarcosine dehydrogenase Homo sapiens 7-10 10479296-0 1999 Design, synthesis, and biological evaluation of novel non-piperazine analogues of 1-[2-(diphenylmethoxy)ethyl]- and 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazines as dopamine transporter inhibitors. Piperazine 58-68 solute carrier family 6 member 3 Homo sapiens 189-209 10386927-1 1999 Combinatorial synthesis of N,N"-di(Boc)-Protected guanidines containing piperazine and pyrrolidine scaffolds has been developed. Piperazine 72-82 BOC cell adhesion associated, oncogene regulated Homo sapiens 35-38 10428371-0 1999 Design and synthesis of thrombin receptor-derived nonpeptide mimetics utilizing a piperazine scaffold. Piperazine 82-92 coagulation factor II (thrombin) receptor Rattus norvegicus 24-41 9822553-7 1998 The simultaneous replacement of both piperazine and furan rings of 1 gave 8 which resulted in a potent, selective alpha1B-adrenoreceptor antagonist (85- and 15-fold more potent than at alpha1A- and alpha1D-subtypes, respectively). Piperazine 37-47 adrenoceptor alpha 1B Homo sapiens 114-136 9873573-2 1998 Bioisosteric replacement of the C-6 carbon atom in piperidine I and piperazine II with S, O, and N heteroatoms is described. Piperazine 68-78 complement C6 Homo sapiens 32-35