PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 27190598-6 2016 Generation of a library of molecules resulted in the identification of the most selective inhibitor of SphK1 reported to date (705-fold selectivity over SphK2), and we found that potency and selectivity vary significantly depending on the particular oxadiazole isomer employed. Oxadiazoles 250-260 sphingosine kinase 1 Homo sapiens 103-108 27149363-3 2016 Current study explores the alpha-glucosidase inhibition of a hybrid class of compounds of oxadiazole and benzofurans. Oxadiazoles 90-100 sucrase-isomaltase Homo sapiens 27-44 26845138-6 2016 To circumvent this problem, a lot of scientists in the world synthesized a series of cis-restricted CA-4 analogs, where the double bond has been replaced by introduction of non-heterocyclic groups or heterocyclic groups like beta -lactam and oxadiazole. Oxadiazoles 242-252 carbonic anhydrase 4 Homo sapiens 100-104 26183542-0 2015 Synthesis of new oxadiazole derivatives as alpha-glucosidase inhibitors. Oxadiazoles 17-27 sucrase-isomaltase Homo sapiens 43-60 26526743-0 2015 Synthesis of novel benzohydrazone-oxadiazole hybrids as beta-glucuronidase inhibitors and molecular modeling studies. Oxadiazoles 34-44 glucuronidase beta Homo sapiens 56-74 26178333-0 2015 Prospective QSAR-Based Prediction Models with Pharmacophore Studies of Oxadiazole-Substituted alpha-Isopropoxy Phenylpropanoic Acids with Dual Activators of PPARalpha and PPARgamma. Oxadiazoles 71-81 peroxisome proliferator activated receptor alpha Homo sapiens 157-166 26178333-0 2015 Prospective QSAR-Based Prediction Models with Pharmacophore Studies of Oxadiazole-Substituted alpha-Isopropoxy Phenylpropanoic Acids with Dual Activators of PPARalpha and PPARgamma. Oxadiazoles 71-81 peroxisome proliferator activated receptor gamma Homo sapiens 171-180 26178333-1 2015 A series of oxadiazole-substituted [Formula: see text]-isopropoxy phenylpropanoic acids with dual activators of PPARalpha and PPARgamma derivatives were subjected to two-dimensional and k-Nearest Neighbors molecular field analysis. Oxadiazoles 12-22 peroxisome proliferator activated receptor alpha Homo sapiens 112-121 26178333-1 2015 A series of oxadiazole-substituted [Formula: see text]-isopropoxy phenylpropanoic acids with dual activators of PPARalpha and PPARgamma derivatives were subjected to two-dimensional and k-Nearest Neighbors molecular field analysis. Oxadiazoles 12-22 peroxisome proliferator activated receptor gamma Homo sapiens 126-135 26726422-1 2015 Novel thermally activated delayed fluorescence (TADF) materials (ACR-OXD, 2ACR-OXD) with 9,10-dihydro-9,9-dimethylacridine (ACR) as an electron donor and oxadiazole derivative (OXD) as an electron acceptor were designed and theoretically investigated for blue OLED emitter. Oxadiazoles 154-164 acrosin Homo sapiens 65-68 26148672-0 2015 Quantitative and qualitative analysis of the novel antitumor 1,3,4-oxadiazole derivative (GLB) and its metabolites using HPLC-UV and UPLC-QTOF-MS. Fructose-based 3-acetyl-2,3-dihydro-1,3,4-oxadiazole (GLB) is a novel antitumor agent and belongs to glycosylated spiro-heterocyclic oxadiazole scaffold derivative. Oxadiazoles 67-77 dicarbonyl and L-xylulose reductase Rattus norvegicus 90-93 25643074-6 2015 Surprisingly, homologation with a single methylene unit between the oxadiazole and heterocyclic ring afforded a SphK1-selective inhibitor in SLP7111228 (Ki = 48 nM), which also decreased S1P levels in cultured U937 cells. Oxadiazoles 68-78 sphingosine kinase 1 Homo sapiens 112-117 25643074-4 2015 Herein, we report the design, synthesis, and structure-activity relationship studies of guanidine-based SphK inhibitors bearing an oxadiazole ring in the scaffold. Oxadiazoles 131-141 sphingosine kinase 1 Homo sapiens 104-108 25671290-0 2015 Synthesis, SAR, and series evolution of novel oxadiazole-containing 5-lipoxygenase activating protein inhibitors: discovery of 2-[4-(3-{(r)-1-[4-(2-amino-pyrimidin-5-yl)-phenyl]-1-cyclopropyl-ethyl}-[1,2,4]oxadiazol-5-yl)-pyrazol-1-yl]-N,N-dimethyl-acetamide (BI 665915). Oxadiazoles 46-56 arachidonate 5-lipoxygenase Homo sapiens 68-82 25671290-1 2015 The synthesis, structure-activity relationship (SAR), and evolution of a novel series of oxadiazole-containing 5-lipoxygenase-activating protein (FLAP) inhibitors are described. Oxadiazoles 89-99 arachidonate 5-lipoxygenase Homo sapiens 111-125 25452003-0 2014 DeltaF508-CFTR correctors: synthesis and evaluation of thiazole-tethered imidazolones, oxazoles, oxadiazoles, and thiadiazoles. Oxadiazoles 97-108 CF transmembrane conductance regulator Homo sapiens 10-14 25255433-0 2014 Design, synthesis, in silico molecular docking and biological evaluation of novel oxadiazole based thiazolidine-2,4-diones bis-heterocycles as PPAR-gamma agonists. Oxadiazoles 82-92 peroxisome proliferator activated receptor gamma Homo sapiens 143-153 25303727-0 2014 Design and synthesis of benzimidazole analogs endowed with oxadiazole as selective COX-2 inhibitor. Oxadiazoles 59-69 mitochondrially encoded cytochrome c oxidase II Homo sapiens 83-88 23143678-3 2013 We have recently realized a series of new inhibitors based on the 4-hydroxy-1,2,5-oxadiazole ring, whose activity profile was found to be closely dependent on the degree of fluorine substitution at the phenyl ring adjacent to the oxadiazole moiety; a positive influence of fluorine on the DHODH inhibitory potency was observed previously [Baumgartner et al. Oxadiazoles 82-92 dihydroorotate dehydrogenase (quinone) Homo sapiens 289-294 25151088-0 2014 Oxadiazoles and thiadiazoles: novel alpha-glucosidase inhibitors. Oxadiazoles 0-11 sucrase-isomaltase Homo sapiens 36-53 25151088-1 2014 Oxadiazoles and thiadiazoles 1-37 were synthesized and evaluated for the first time for their alpha-glucosidase inhibitory activities. Oxadiazoles 0-11 sucrase-isomaltase Homo sapiens 94-111 24081608-1 2014 The binding modes of 42 oxadiazole derivates inside glycogen synthase kinase 3 beta (GSK3beta were determined using docking experiments; thus, the preferred active conformations of these inhibitors are proposed. Oxadiazoles 24-34 glycogen synthase kinase 3 beta Homo sapiens 52-83 24081608-1 2014 The binding modes of 42 oxadiazole derivates inside glycogen synthase kinase 3 beta (GSK3beta were determined using docking experiments; thus, the preferred active conformations of these inhibitors are proposed. Oxadiazoles 24-34 glycogen synthase kinase 3 beta Homo sapiens 85-93 24072592-4 2013 We show that the resulting oxadiazole-substituted aza-benzimidazole is a potent and ligand efficient S6 kinase inhibitor, which blocks the phosphorylation of RPS6 at Ser235/236 in TSC negative HCV29 human bladder cancer cells by inhibiting S6 kinase activity and thus provides a useful tool compound to investigate the function of S6 kinases. Oxadiazoles 27-37 ribosomal protein S6 Homo sapiens 158-162 22749643-0 2013 Structure-based optimization of oxadiazole-based GSK-3 inhibitors. Oxadiazoles 32-42 glycogen synthase kinase 3 beta, genome duplicate a Danio rerio 49-54 22749643-4 2013 Particularly, the oxadiazole scaffold provided potent and selective GSK-3 inhibitors. Oxadiazoles 18-28 glycogen synthase kinase 3 beta, genome duplicate a Danio rerio 68-73 25183350-0 2014 Prospective QSAR-based prediction models with pharmacophore studies of oxadiazole-substituted alpha-isopropoxy phenylpropanoic acids on with dual activators of PPARalpha and PPARgamma A series of oxadiazole-substituted alpha-isopropoxy phenylpropanoic acids with dual activators of PPARalpha and PPARgamma derivatives were subjected to two dimensional and k-nearest neighbour Molecular field analysis. Oxadiazoles 71-81 peroxisome proliferator activated receptor alpha Homo sapiens 160-169 25183350-0 2014 Prospective QSAR-based prediction models with pharmacophore studies of oxadiazole-substituted alpha-isopropoxy phenylpropanoic acids on with dual activators of PPARalpha and PPARgamma A series of oxadiazole-substituted alpha-isopropoxy phenylpropanoic acids with dual activators of PPARalpha and PPARgamma derivatives were subjected to two dimensional and k-nearest neighbour Molecular field analysis. Oxadiazoles 71-81 peroxisome proliferator activated receptor gamma Homo sapiens 174-183 24979042-1 2014 We present here a simple, milder, and environmentally benign heterogeneous catalytic method for the transformation of tetrazines to oxadiazole derivatives at room temperature (25 C) using our earlier synthesized iron-squarate based 3D metal organic framework, [Fe3(OH)3(C4O4)(C4O4)0.5]n (FeSq-MOF). Oxadiazoles 132-142 lysine acetyltransferase 8 Homo sapiens 294-297 24081608-0 2014 Docking and quantitative structure-activity relationship of oxadiazole derivates as inhibitors of GSK3beta. Oxadiazoles 60-70 glycogen synthase kinase 3 beta Homo sapiens 98-106 24138603-3 2013 We show that the presence of CsF/Al at cathodes not only improves electron transport in oxadiazole-containing electron transport layers (ETLs), but also facilitates electron injection through the reacted oxadiazole moiety to reduce interface resistance, which results in the enhancement of current efficiency. Oxadiazoles 88-98 colony stimulating factor 2 Homo sapiens 29-32 24138603-3 2013 We show that the presence of CsF/Al at cathodes not only improves electron transport in oxadiazole-containing electron transport layers (ETLs), but also facilitates electron injection through the reacted oxadiazole moiety to reduce interface resistance, which results in the enhancement of current efficiency. Oxadiazoles 204-214 colony stimulating factor 2 Homo sapiens 29-32 23504218-1 2013 An oxadiazole derivative(OXD) containing symmetrical pyridine-2-formamidophenyl-binded moiety was synthesised as fluorescence turn-on sensor OA1. Oxadiazoles 3-13 OA1 Homo sapiens 141-144 23469385-7 2010 The first oxadiazole-based probe (ML236, PubChem CID665654) is potent (35 nM) in a B-cell line and >400-fold selective over both the NF-kappaB activation in T-cells and against TNFalpha-mediated NF-kappaB activation. Oxadiazoles 10-20 tumor necrosis factor Homo sapiens 180-188 22608962-0 2012 Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes. Oxadiazoles 55-65 diacylglycerol O-acyltransferase 1 Homo sapiens 66-72 22683241-0 2012 Synthesis and biological evaluation of isoxazole, oxazole, and oxadiazole containing heteroaryl analogs of biaryl ureas as DGAT1 inhibitors. Oxadiazoles 63-73 diacylglycerol O-acyltransferase 1 Mus musculus 123-128 21621412-5 2011 Docking studies of triazole-linked reduced amide isostere A3Z10 and potent oxadiazole-linked tertiary carbinamine 2a with BACE1 suggests that the docking poses of A3Z10 and 2a in the active sites are quite similar, with one exception. Oxadiazoles 75-85 beta-secretase 1 Homo sapiens 122-127 21824692-1 2011 In this study novel ligands of the translocator protein (TSPO), characterized by a five-membered aromatic heterocycle (i.e. oxazole, isoxazole, oxadiazole), a phenyl ring, and an amide side chain of carboxy or acetic type, were designed using a previously reported pharmacophore/topological model. Oxadiazoles 144-154 translocator protein Homo sapiens 35-55 21824692-1 2011 In this study novel ligands of the translocator protein (TSPO), characterized by a five-membered aromatic heterocycle (i.e. oxazole, isoxazole, oxadiazole), a phenyl ring, and an amide side chain of carboxy or acetic type, were designed using a previously reported pharmacophore/topological model. Oxadiazoles 144-154 translocator protein Homo sapiens 57-61 21316962-2 2011 The oral bioavailability of these compounds could be dramatically improved by optimization studies of the side chains attached to the indole and oxadiazole cores, leading to identification of a CB1 receptor agonist with good oral activity in a range of preclinical models of antinociception and antihyperalgesia. Oxadiazoles 145-155 cannabinoid receptor 1 Homo sapiens 194-197 20727744-1 2010 With a small series of compounds we demonstrated the variability in the core region of the human histamine H(3) receptor (hH(3)R) antagonist structural blueprint by introducing polar azole groups (oxazole, oxadiazole, thiazole and triazole). Oxadiazoles 206-216 histamine receptor H3 Homo sapiens 97-120 20965619-7 2010 We had noticed that compounds (AB13, AB20) bearing OH group at one of the phenyl ring of oxadiazole exhibited good antimicrobial properties and their drug-likeness model score were also predicted maximum among the series. Oxadiazoles 89-99 NBPF member 1 Homo sapiens 31-35 20727744-1 2010 With a small series of compounds we demonstrated the variability in the core region of the human histamine H(3) receptor (hH(3)R) antagonist structural blueprint by introducing polar azole groups (oxazole, oxadiazole, thiazole and triazole). Oxadiazoles 206-216 histamine receptor H3 Homo sapiens 122-128 20055416-4 2010 Our data revealed that those EA oxadiazole analogues had improved antiproliferative activity and most of them had similar or better inhibitory effects on GST P1-1 activity than EA. Oxadiazoles 32-42 glutathione S-transferase pi 1 Homo sapiens 154-162 20055416-7 2010 Our data suggest that these EA oxadiazole analogues are promising antitumor agents that may act through GST P1-1 inhibition-dependent and/or -independent pathways. Oxadiazoles 31-41 glutathione S-transferase pi 1 Homo sapiens 104-112 19197923-2 2009 This effort identified key substituents in the 3-position of oxadiazole that engendered either mGluR5 ago-potentiation or pure mGluR5 positive allosteric modulation. Oxadiazoles 61-71 glutamate receptor, ionotropic, kainate 1 Mus musculus 95-101 20036129-0 2010 Synthesis and biological evaluation of oxadiazole derivatives as inhibitors of soluble guanylyl cyclase. Oxadiazoles 39-49 guanylate cyclase 1 soluble subunit beta 2 Rattus norvegicus 79-103 19637873-3 2009 Detailed investigation of the SAR series subsequently revealed that many members of the oxadiazole class (and surprisingly also 1) act via divergent modes of inhibition (competitive or via colloidal aggregation) depending on the assay conditions employed. Oxadiazoles 88-98 sarcosine dehydrogenase Homo sapiens 30-33 19370348-15 2009 We postulate that diminished HIF-1alpha nuclear presence in oxadiazole treated EAT cells could be responsible for decreased VEGF expression and antiangiogenic effects. Oxadiazoles 60-70 hypoxia inducible factor 1, alpha subunit Mus musculus 29-39 19370348-15 2009 We postulate that diminished HIF-1alpha nuclear presence in oxadiazole treated EAT cells could be responsible for decreased VEGF expression and antiangiogenic effects. Oxadiazoles 60-70 vascular endothelial growth factor A Mus musculus 124-128 19637873-2 2009 Chemical optimization of 1 led to a series of oxadiazoles possessing interpretable SAR and potencies as much as 500-fold greater than 1. Oxadiazoles 46-57 sarcosine dehydrogenase Homo sapiens 83-86 19197923-2 2009 This effort identified key substituents in the 3-position of oxadiazole that engendered either mGluR5 ago-potentiation or pure mGluR5 positive allosteric modulation. Oxadiazoles 61-71 glutamate receptor, ionotropic, kainate 1 Mus musculus 127-133 17723300-0 2007 Pyrrolidine-carboxamides and oxadiazoles as potent hNK1 antagonists. Oxadiazoles 29-40 beta-1,3-glucuronyltransferase 1 Homo sapiens 51-55 18642893-0 2008 Oxadiazole-carbonylaminothioureas as SIRT1 and SIRT2 inhibitors. Oxadiazoles 0-10 sirtuin 1 Homo sapiens 37-42 18642893-0 2008 Oxadiazole-carbonylaminothioureas as SIRT1 and SIRT2 inhibitors. Oxadiazoles 0-10 sirtuin 2 Homo sapiens 47-52 19802367-2 2009 These compounds were prepared in an effort to probe the SAR around the phenyl substituent and oxadiazole core for our studies toward thioredoxin-glutathione reductase (TGR) inhibition and anti-schistosomal activity. Oxadiazoles 94-104 thioredoxin reductase 3 Homo sapiens 133-166 19802367-2 2009 These compounds were prepared in an effort to probe the SAR around the phenyl substituent and oxadiazole core for our studies toward thioredoxin-glutathione reductase (TGR) inhibition and anti-schistosomal activity. Oxadiazoles 94-104 thioredoxin reductase 3 Homo sapiens 168-171 19200745-2 2009 Here we report design, synthesis and structure-activity relationships of a novel series of oxadiazole derivatives as GSK-3beta inhibitors. Oxadiazoles 91-101 glycogen synthase kinase 3 beta Homo sapiens 117-126 19147366-7 2009 Finally, substitution of oxadiazoles for the furan ring abolished affinity for the KOPR. Oxadiazoles 25-36 opioid receptor kappa 1 Homo sapiens 83-87 19200038-0 2009 Interaction models of a series of oxadiazole-substituted alpha-isopropoxy phenylpropanoic acids against PPARalpha and PPARgamma: molecular modeling and comparative molecular similarity indices analysis studies. Oxadiazoles 34-44 peroxisome proliferator activated receptor alpha Homo sapiens 104-113 19200038-0 2009 Interaction models of a series of oxadiazole-substituted alpha-isopropoxy phenylpropanoic acids against PPARalpha and PPARgamma: molecular modeling and comparative molecular similarity indices analysis studies. Oxadiazoles 34-44 peroxisome proliferator activated receptor gamma Homo sapiens 118-127 19200038-1 2009 Molecular recognition of a series of oxadiazole-substituted alpha-isopropoxy phenylpropanoic acids by PPARalpha and PPARgamma was investigated by using molecular modeling and 3D-QSAR analyses. Oxadiazoles 37-47 peroxisome proliferator activated receptor alpha Homo sapiens 102-111 19200038-1 2009 Molecular recognition of a series of oxadiazole-substituted alpha-isopropoxy phenylpropanoic acids by PPARalpha and PPARgamma was investigated by using molecular modeling and 3D-QSAR analyses. Oxadiazoles 37-47 peroxisome proliferator activated receptor gamma Homo sapiens 116-125 19200038-5 2009 The oxadiazole-ring-related hydrogen bond interactions well elucidate the structural features governing the different binding behavior of these agonists against PPARalpha and PPARgamma. Oxadiazoles 4-14 peroxisome proliferator activated receptor alpha Homo sapiens 161-170 19200038-5 2009 The oxadiazole-ring-related hydrogen bond interactions well elucidate the structural features governing the different binding behavior of these agonists against PPARalpha and PPARgamma. Oxadiazoles 4-14 peroxisome proliferator activated receptor gamma Homo sapiens 175-184 19053260-0 2008 Molecular design of new inhibitors of peroxidase activity of cytochrome c/cardiolipin complexes: fluorescent oxadiazole-derivatized cardiolipin. Oxadiazoles 109-119 cytochrome c, somatic Homo sapiens 61-73 18951019-4 2008 An oxadiazole moiety behaves as a bioisostere for the hydroxamate group, leading to a more metabolically stable and efficacious MEK inhibitor. Oxadiazoles 3-13 mitogen-activated protein kinase kinase 7 Homo sapiens 128-131 18680277-2 2008 Herein we describe the discovery of a novel class of oxadiazole derivatives from which potent and selective CB2 agonist leads were developed. Oxadiazoles 53-63 cannabinoid receptor 2 Rattus norvegicus 108-111 17723300-3 2007 Oxadiazole analog 22 was determined to have excellent hNK(1) binding affinity, functional activity, and a good PD response in vivo. Oxadiazoles 0-10 beta-1,3-glucuronyltransferase 1 Homo sapiens 54-59 16919457-0 2006 Discovery of potent, selective, and orally bioavailable oxadiazole-based dipeptidyl peptidase IV inhibitors. Oxadiazoles 56-66 dipeptidyl peptidase 4 Homo sapiens 73-96 17574410-1 2007 A novel series of oxadiazole EP1 receptor antagonists was identified by replacing the amide of a known glycine sulfonamide derivative with a 1,3,4-oxadiazole. Oxadiazoles 18-28 prostaglandin E receptor 1 Homo sapiens 29-32 16919457-1 2006 A novel series of oxadiazole based amides have been shown to be potent DPP-4 inhibitors. Oxadiazoles 18-28 dipeptidyl peptidase 4 Homo sapiens 71-76 11527737-0 2001 Identification of a series of oxadiazole-substituted alpha-isopropoxy phenylpropanoic acids with activity on PPARalpha, PPARgamma, and PPARdelta. Oxadiazoles 30-40 peroxisome proliferator activated receptor alpha Homo sapiens 109-118 16602792-1 2006 One nanosized oxadiazole bridging ligand, bis(3-acetylenylphenyl-(4-cyanophenyl))oxadiazole (L11), was designed and synthesized by the reaction of bis(3-iodophenyl)oxadiazole with 4-cyanophenylacetylene via a Sonogashira-Hagihara cross-coupling reaction. Oxadiazoles 14-24 immunoglobulin kappa variable 1-6 Homo sapiens 93-96 16602792-5 2006 In this Ag(I)-L11 system, the conformation of L11 is versatile because of the conformational rotation around the central oxadiazole moiety and depends greatly on the counterion and solvent system used in the formation of the complexes. Oxadiazoles 121-131 immunoglobulin kappa variable 1-6 Homo sapiens 14-17 16602792-5 2006 In this Ag(I)-L11 system, the conformation of L11 is versatile because of the conformational rotation around the central oxadiazole moiety and depends greatly on the counterion and solvent system used in the formation of the complexes. Oxadiazoles 121-131 immunoglobulin kappa variable 1-6 Homo sapiens 46-49 16162010-5 2005 The diacylhydrazine was found to be superior over the oxadiazole as an amide bond replacement in the Plm I and II inhibitors studied. Oxadiazoles 54-64 FXYD domain containing ion transport regulator 1 Homo sapiens 101-104 11527737-0 2001 Identification of a series of oxadiazole-substituted alpha-isopropoxy phenylpropanoic acids with activity on PPARalpha, PPARgamma, and PPARdelta. Oxadiazoles 30-40 peroxisome proliferator activated receptor gamma Homo sapiens 120-129 11527737-0 2001 Identification of a series of oxadiazole-substituted alpha-isopropoxy phenylpropanoic acids with activity on PPARalpha, PPARgamma, and PPARdelta. Oxadiazoles 30-40 peroxisome proliferator activated receptor delta Homo sapiens 135-144 11514143-3 2001 The synthesized oxadiazoles were evaluated for their affinity to the DAT and their ability to inhibit monoamine reuptake at the DAT, NET, and 5HTT. Oxadiazoles 16-27 solute carrier family 6 member 3 Homo sapiens 69-72 11514143-3 2001 The synthesized oxadiazoles were evaluated for their affinity to the DAT and their ability to inhibit monoamine reuptake at the DAT, NET, and 5HTT. Oxadiazoles 16-27 solute carrier family 6 member 3 Homo sapiens 128-131 11514143-4 2001 The results show that affinity to the DAT and ability to inhibit the reuptake at the DAT, NET, and 5HTT is a function of the size of the substituent in the oxadiazole ring. Oxadiazoles 156-166 solute carrier family 6 member 3 Homo sapiens 38-41 11514143-4 2001 The results show that affinity to the DAT and ability to inhibit the reuptake at the DAT, NET, and 5HTT is a function of the size of the substituent in the oxadiazole ring. Oxadiazoles 156-166 solute carrier family 6 member 3 Homo sapiens 85-88 10395735-6 1999 Nonpeptidic HNE inhibitors containing the oxadiazole heterocycle displayed promising oral bioavailability. Oxadiazoles 42-52 elastase, neutrophil expressed Homo sapiens 12-15 8496922-2 1993 Modifications of the oxadiazole 3-substituent, length of the linking chain (n), and the amine substituents are explored and reveal a large binding pocket in the 5-HT1D receptor domain. Oxadiazoles 21-31 5-hydroxytryptamine receptor 1D Homo sapiens 161-167 34426156-0 2021 Novel 1,3,4-thiadiazole/oxadiazole-linked honokiol derivatives suppress cancer via inducing PI3K/Akt/mTOR-dependent autophagy. Oxadiazoles 24-34 AKT serine/threonine kinase 1 Homo sapiens 97-100 18802648-1 2008 A novel series of oxadiazoles as CB1 cannabinoid receptor antagonists. Oxadiazoles 18-29 cannabinoid receptor 1 Homo sapiens 33-36 18802648-2 2008 Based on the bioisosteric replacement of the pyrazole C3-carboxamide of rimonabant with a 5-alkyl oxadiazole ring, a novel class of oxadiazole derivatives with promising biological activity towards CB1 receptors was discovered. Oxadiazoles 98-108 cannabinoid receptor 1 Homo sapiens 198-201 34426156-0 2021 Novel 1,3,4-thiadiazole/oxadiazole-linked honokiol derivatives suppress cancer via inducing PI3K/Akt/mTOR-dependent autophagy. Oxadiazoles 24-34 mechanistic target of rapamycin kinase Homo sapiens 101-105 34424718-1 2021 It has been reported that DIC can react with OxymaPure to render an oxadiazole compound with the concomitant formation of HCN. Oxadiazoles 68-78 metastasis associated lung adenocarcinoma transcript 1 Homo sapiens 122-125 34275792-5 2021 The hydrazides were cyclized with CS2 in the presence of KOH to yield corresponding oxadiazoles (4a-f). Oxadiazoles 84-95 chorionic somatomammotropin hormone 2 Homo sapiens 34-37 34089945-3 2021 Herein, 4-benzyl-2-benzylthio-5-methyl-1H-imidazole (2a) and 4-benzyl-5-methyl-2-((2,6-difluorobenzyl)thio)-1H-imidazole (2d) from a group of thirty imidazole-bearing compounds showed greater STAT3 inhibition than their lead compounds VS1 and the oxadiazole derivative MD77. Oxadiazoles 247-257 signal transducer and activator of transcription 3 Homo sapiens 192-197 34251799-1 2021 A series of oxadiazole derivatives were synthesized and evaluated as 5-hydroxytryptamine-4 receptor (5-HT4R) partial agonists for the treatment of cognitive deficits associated with Alzheimer"s disease. Oxadiazoles 12-22 5-hydroxytryptamine receptor 4 Homo sapiens 69-99 34251799-1 2021 A series of oxadiazole derivatives were synthesized and evaluated as 5-hydroxytryptamine-4 receptor (5-HT4R) partial agonists for the treatment of cognitive deficits associated with Alzheimer"s disease. Oxadiazoles 12-22 5-hydroxytryptamine receptor 4 Homo sapiens 101-107 34602444-0 2021 In-vitro cytotoxic evaluation of newly designed ciprofloxacin-oxadiazole hybrids against human liver tumor cell line (Huh7). Oxadiazoles 62-72 MIR7-3 host gene Homo sapiens 118-122 35189320-1 2022 A series of novel spirocyclic DGAT1 inhibitors containing the oxadiazole motif were designed and synthesized for biological evaluation. Oxadiazoles 62-72 diacylglycerol O-acyltransferase 1 Mus musculus 30-35 35455397-11 2022 Many oxadiazoles showed lower IC50 values against AChE than established drug rivastigmine. Oxadiazoles 5-16 acetylcholinesterase (Cartwright blood group) Homo sapiens 50-54 33494672-6 2021 Results and Conclusion: It was observed that structures of the GSK-3 inhibitors comprised of benzopyridine, benzthiazole, pyrazole, pyrazine, dioxolo-benzoxazin, oxadiazole, benzimidazole in the skeletal with cyclopropylamide, phenyl carbamothioate, 3-[(propan-2-yl)oxy]propan-1-amine in side chain. Oxadiazoles 162-172 glycogen synthase kinase 3 beta Mus musculus 63-68 1179029-7 1975 The in vitro protection of trypsin-induced hydrolysis of bovine serum albumin, unlike antiinflammatory activity, was greater with oxadiazoles (30-90%) than the precursor thiosemicarbazides (4-50%) at a final concentration of 1 mM. Oxadiazoles 130-141 albumin Rattus norvegicus 64-77 35163965-0 2022 Design and Activity of Novel Oxadiazole Based Compounds That Target Poly(ADP-ribose) Polymerase. Oxadiazoles 29-39 poly(ADP-ribose) polymerase 1 Homo sapiens 68-95 35163965-2 2022 Herein, oxadiazole based ligands that are predicted to target PARP-1 have been synthesized and screened for the loss of cell viability in mammary carcinoma cells, wherein seven compounds were observed to possess significant IC50 values in the range of 1.4 to 25 microM. Oxadiazoles 8-18 poly(ADP-ribose) polymerase 1 Homo sapiens 62-68 35163965-7 2022 Finally, in silico analysis demonstrated binding of compound 5s towardsthe catalytic site of PARP-1, indicating that these novel oxadiazoles synthesized herein may serve as exemplars for the development of new therapeutics in cancer. Oxadiazoles 129-140 poly(ADP-ribose) polymerase 1 Homo sapiens 93-99 33859800-4 2021 We describe the development of a novel class of oxadiazole KNa1.1 inhibitors, leading to the discovery of compound 31 that reduced seizures and interictal spikes in a mouse model of KCNT1 GoF. Oxadiazoles 48-58 potassium channel, subfamily T, member 1 Mus musculus 182-187 32854311-1 2020 Analgesic and anti-inflammatory properties mediated by the kappa opioid receptor (KOR) have been reported for oxadiazole imidazodiazepines. Oxadiazoles 110-120 opioid receptor kappa 1 Homo sapiens 59-80 33139114-11 2021 Ataluren, an oxadiazole compound that promotes read-through and expression of dystrophin in patients with Duchenne muscular dystrophy, bears some structural similarity to SRI-22819. Oxadiazoles 13-23 dystrophin Homo sapiens 78-88 33360082-3 2021 Aiming at the elucidation of MAO-B inhibitors with 1,3,4-oxadiazole scaffolds, we make a comprehensive update on the new and old chemical methods employed for the synthesis of the unsymmetrical oxadiazole derivatives that lead to high yield compounds. Oxadiazoles 57-67 monoamine oxidase B Homo sapiens 29-34 33360082-4 2021 We summarize a state of the selective MAO-B inhibitors with oxadiazole scaffold, describing the results, structures, structure-activity relationships (SARs) and medicinal chemistry strategies over the years. Oxadiazoles 60-70 monoamine oxidase B Homo sapiens 38-43 33360082-5 2021 The analysis of the recent papers would facilitate tracking the increasing number of oxadiazole derivatives as new chemical spaces with MAO-B inhibitory potential designed to ensure the safe use of the compounds and elimination of the unwanted drug-drug interactions. Oxadiazoles 85-95 monoamine oxidase B Homo sapiens 136-141 33256166-0 2020 Design, Synthesis and Evaluation of New Bioactive Oxadiazole Derivatives as Anticancer Agents Targeting Bcl-2. Oxadiazoles 50-60 BCL2 apoptosis regulator Homo sapiens 104-109 32854311-1 2020 Analgesic and anti-inflammatory properties mediated by the kappa opioid receptor (KOR) have been reported for oxadiazole imidazodiazepines. Oxadiazoles 110-120 opioid receptor kappa 1 Homo sapiens 82-85 31945272-0 2020 From Oxadiazole to Triazole Analogues: Optimization toward a Dual Orexin Receptor Antagonist with Improved in vivo Efficacy in Dogs. Oxadiazoles 5-15 hypocretin neuropeptide precursor Canis lupus familiaris 66-72 32325339-0 2020 Exploiting oxadiazole-sulfonamide hybrids as new structural leads to combat diabetic complications via aldose reductase inhibition. Oxadiazoles 11-21 aldo-keto reductase family 1 member B Homo sapiens 103-119 32451633-2 2020 The comparative study of optoelectronic properties indicates that thiadiazole with pyridine units containing molecules (M6b) exhibit lower energy of highest occupied molecular orbital (HOMO) and lowest unoccupied molecular orbital (LUMO) energy levels than those of oxadiazole and pyridine containing units (M6b). Oxadiazoles 266-276 glycoprotein M6B Homo sapiens 120-123 32631535-0 2020 Exploring the newer oxadiazoles as real inhibitors of human SIRT2 in hepatocellular cancer cells. Oxadiazoles 20-31 sirtuin 2 Homo sapiens 60-65 32027778-5 2020 Several molecules containing a S-Et- or a S-Me-Itc moiety and mainly belonging to the dipeptide-like and 1,2,4-oxadiazole series were shown to inhibit nNOS and iNOS with IC50 in the 1-50 muM range. Oxadiazoles 105-121 nitric oxide synthase 1 Rattus norvegicus 151-155 32027778-5 2020 Several molecules containing a S-Et- or a S-Me-Itc moiety and mainly belonging to the dipeptide-like and 1,2,4-oxadiazole series were shown to inhibit nNOS and iNOS with IC50 in the 1-50 muM range. Oxadiazoles 105-121 nitric oxide synthase 2 Rattus norvegicus 160-164 31684051-0 2019 Development of Oxadiazole-Based ODZ10117 as a Small-Molecule Inhibitor of STAT3 for Targeted Cancer Therapy. Oxadiazoles 15-25 signal transducer and activator of transcription 3 Homo sapiens 74-79 31757525-0 2020 Design, synthesis and biological evaluation of new Axl kinase inhibitors containing 1,3,4-oxadiazole acetamide moiety as novel linker. Oxadiazoles 86-110 AXL receptor tyrosine kinase Homo sapiens 51-54 31195948-1 2020 BACKGROUND: In the recent past, we had synthesized and reported different derivatives of oxadiazoles as potential alpha-glucosidase inhibitors. Oxadiazoles 89-100 sucrase-isomaltase Homo sapiens 114-131 31622615-3 2020 Ursolic acid hydrazide provided access to oxadiazoles attached directly to C-17 of the ursane core, but synthesis of structurally related 3-mercapto-1,2,4-triazoles was not possible in this way due to steric hindrance of the triterpenoid. Oxadiazoles 42-53 cytokine like 1 Homo sapiens 75-79 31539778-0 2019 New oxadiazoles with selective-COX-2 and EGFR dual inhibitory activity: Design, synthesis, cytotoxicity evaluation and in silico studies. Oxadiazoles 4-15 mitochondrially encoded cytochrome c oxidase II Homo sapiens 31-36 31539778-0 2019 New oxadiazoles with selective-COX-2 and EGFR dual inhibitory activity: Design, synthesis, cytotoxicity evaluation and in silico studies. Oxadiazoles 4-15 epidermal growth factor receptor Homo sapiens 41-45 31999451-3 2020 The representative compound 8u bound effectively to IDO1, with greater inhibitory activity relative to the commercial IDO1 inhibitor 4-amino-N-(3-chloro-4-fluorophenyl)-N"-hydroxy-1, 2, 5-oxadiazole-3-carboximidamide (IDO5L) in addition to efficient suppression of nuclear translocation of STAT3. Oxadiazoles 186-216 indoleamine 2,3-dioxygenase 1 Homo sapiens 52-56 31865813-5 2020 The recent invention of oxadiazole-based ligands by pharmaceutical companies may provide a new opportunity to optimize the druglike properties of HDAC6 inhibitors for the treatment of neurodegenerative diseases. Oxadiazoles 24-34 histone deacetylase 6 Homo sapiens 146-151 31589148-6 2019 Two L5 ligands are bound to two Ag1 centres through two oxadiazole N and two pyridyl N atoms to form a macrocycle. Oxadiazoles 56-68 NBPF member 10 Homo sapiens 32-35 31589148-7 2019 The other two oxadiazole N atoms coordinate to the two Ag2 centres of the Ag2(O2CCF3)4 dimer. Oxadiazoles 14-24 anterior gradient 2, protein disulphide isomerase family member Homo sapiens 55-58 31589148-7 2019 The other two oxadiazole N atoms coordinate to the two Ag2 centres of the Ag2(O2CCF3)4 dimer. Oxadiazoles 14-24 anterior gradient 2, protein disulphide isomerase family member Homo sapiens 74-77 31288965-0 2019 Optimization of oxadiazole derivatives with a spirocyclic cyclohexane structure as novel GPR119 agonists. Oxadiazoles 16-26 G protein-coupled receptor 119 Rattus norvegicus 89-95 31196753-0 2019 Synthesis of oxadiazole-coupled-thiadiazole derivatives as a potent beta-glucuronidase inhibitors and their molecular docking study. Oxadiazoles 13-23 glucuronidase beta Homo sapiens 68-86 31196753-1 2019 A new series of oxadiazole with thiadiazole moiety (6-27) were synthesized, characterized by different spectroscopic techniques and evaluated for beta-glucuronidase inhibitory potential. Oxadiazoles 16-26 glucuronidase beta Homo sapiens 146-164 31187977-3 2019 In this contribution, a novel BF2-containing TADF molecule of BFOXD, which contains two acceptor fragments of oxadiazole (OXD) and BF2 and one donor unit of 9,9-dimethylacridine, was synthesized and characterized. Oxadiazoles 110-120 forkhead box G1 Homo sapiens 30-33 29803079-0 2018 Synthesis, SAR elucidations and molecular docking study of newly designed isatin based oxadiazole analogs as potent inhibitors of thymidine phosphorylase. Oxadiazoles 87-97 sarcosine dehydrogenase Homo sapiens 11-14 31066976-0 2019 Oxadiazole Derivatives as Dual Orexin Receptor Antagonists: Synthesis, Structure-Activity Relationships, and Sleep-Promoting Properties in Rats. Oxadiazoles 0-10 hypocretin neuropeptide precursor Rattus norvegicus 31-37 31003424-0 2019 Synthesis of Chromen-4-One-Oxadiazole Substituted Analogs as Potent beta-Glucuronidase Inhibitors. Oxadiazoles 27-37 glucuronidase beta Homo sapiens 68-86 31003424-1 2019 Chromen-4-one substituted oxadiazole analogs 1-19 have been synthesized, characterized and evaluated for beta-glucuronidase inhibition. Oxadiazoles 26-36 glucuronidase beta Homo sapiens 105-123 30792038-1 2019 Oxadiazole replacement of an amide linkage in an RARalpha agonist template 1, followed by lead optimisation, has produced a highly potent and selective RARbeta agonist 4-(5-(4,7-dimethylbenzofuran-2-yl)-1,2,4-oxadiazol-3-yl)benzoic acid (10) with good oral bioavailability in the rat and dog. Oxadiazoles 0-10 retinoic acid receptor, alpha Rattus norvegicus 49-57 30792038-1 2019 Oxadiazole replacement of an amide linkage in an RARalpha agonist template 1, followed by lead optimisation, has produced a highly potent and selective RARbeta agonist 4-(5-(4,7-dimethylbenzofuran-2-yl)-1,2,4-oxadiazol-3-yl)benzoic acid (10) with good oral bioavailability in the rat and dog. Oxadiazoles 0-10 retinoic acid receptor, alpha Rattus norvegicus 152-159 30599411-5 2019 In this regard we have synthesized benzothiazole based oxadiazole in search of potent anti-diabetic agent as alpha-glucosidase Inhibitors. Oxadiazoles 55-65 sucrase-isomaltase Homo sapiens 109-126 30599411-6 2019 Benzothiazole based oxadiazole derivatives 1-23 have been synthesized, characterized by 1HNMR, 13CNMR, and MS and evaluated for alpha-glucosidase Inhibition. Oxadiazoles 20-30 sucrase-isomaltase Homo sapiens 128-145 30857263-4 2019 Twenty-two (1-22) analogs of indole based oxadiazole were synthesized and screened for their inhibitory potential against beta-glucuronidase. Oxadiazoles 42-52 glucuronidase beta Homo sapiens 122-140 30591450-2 2019 The aim of this study was to explore the SAR of newly-synthesized oxadiazole derivatives and identify their molecular targets. Oxadiazoles 66-76 sarcosine dehydrogenase Homo sapiens 41-44 30280671-0 2019 3D-QSAR and Molecular Docking Studies on Oxadiazole Substituted Benzimidazole Derivatives: Validation of Experimental Inhibitory Potencies Towards COX-2. Oxadiazoles 41-51 mitochondrially encoded cytochrome c oxidase II Homo sapiens 147-152 30268973-0 2019 Identification and Structure-Activity Relationship (SAR) of potent and selective oxadiazole-based agonists of sphingosine-1-phosphate receptor (S1P1). Oxadiazoles 81-91 sphingosine-1-phosphate receptor 1 Homo sapiens 144-148 30268973-2 2019 In this paper we described a series of oxadiazole-based S1P1 direct-acting agonists disubstituted on terminal benzene ring, with high potency for S1P1 receptor and favorable selectivity against S1P3 receptor. Oxadiazoles 39-49 sphingosine-1-phosphate receptor 1 Homo sapiens 56-60 30268973-2 2019 In this paper we described a series of oxadiazole-based S1P1 direct-acting agonists disubstituted on terminal benzene ring, with high potency for S1P1 receptor and favorable selectivity against S1P3 receptor. Oxadiazoles 39-49 sphingosine-1-phosphate receptor 1 Homo sapiens 146-150 30996787-0 2019 Investigation around the Oxadiazole Core in the Discovery of a New Chemotype of Potent and Selective FXR Antagonists. Oxadiazoles 25-35 nuclear receptor subfamily 1 group H member 4 Homo sapiens 101-104 30192504-3 2018 The oxadiazole compounds doped in hosts (mCP and PPT) emitted from 435 to 474 nm with photoluminescence quantum yields ranging from 14-55%. Oxadiazoles 4-14 CD46 antigen, complement regulatory protein Mus musculus 41-44 30192504-3 2018 The oxadiazole compounds doped in hosts (mCP and PPT) emitted from 435 to 474 nm with photoluminescence quantum yields ranging from 14-55%. Oxadiazoles 4-14 tachykinin precursor 1 Homo sapiens 49-52 30568762-5 2018 Furthermore, docking of 6e/6h into the ATR structure active site revealed that the N1 and N8 atoms in the naphthyridine ring and the hybrid atom in the oxadiazole ring are involved in hydrogen bonding with Val170, Glu168 and Tyr155. Oxadiazoles 152-162 serine/threonine-protein kinase ATR Cricetulus griseus 39-42 28067996-1 2017 A new series of oxadiazoles were designed to act as inhibitors of the anti-apoptotic Bcl-2 protein. Oxadiazoles 16-27 BCL2 apoptosis regulator Homo sapiens 85-90 29223804-0 2018 Oxindole based oxadiazole hybrid analogs: Novel alpha-glucosidase inhibitors. Oxadiazoles 15-25 sucrase-isomaltase Homo sapiens 48-65 29223804-3 2018 Keeping in view the greater importance of alpha-glucosidase inhibitors here in this study we are presenting oxindole based oxadiazoles hybrid analogs (1-20) synthesis, characterized by different spectroscopic techniques including 1H NMR and EI-MS and their alpha-glucosidase inhibitory activity. Oxadiazoles 123-134 sucrase-isomaltase Homo sapiens 42-59 29223804-3 2018 Keeping in view the greater importance of alpha-glucosidase inhibitors here in this study we are presenting oxindole based oxadiazoles hybrid analogs (1-20) synthesis, characterized by different spectroscopic techniques including 1H NMR and EI-MS and their alpha-glucosidase inhibitory activity. Oxadiazoles 123-134 sucrase-isomaltase Homo sapiens 257-274 29960729-0 2018 Design, synthesis, and biological evaluation of novel oxadiazole- and thiazole-based histamine H3R ligands. Oxadiazoles 54-64 histamine receptor H3 Homo sapiens 95-98 29960729-3 2018 This prompted us to design and synthesize azole-based H3R ligands, i.e. having oxadiazole- or thiazole-based core structures. Oxadiazoles 79-89 histamine receptor H3 Homo sapiens 54-57 29966916-0 2018 Design, synthesis, in vitro and in silico evaluation of a new series of oxadiazole-based anticancer agents as potential Akt and FAK inhibitors. Oxadiazoles 72-82 thymoma viral proto-oncogene 1 Mus musculus 120-123 29966916-0 2018 Design, synthesis, in vitro and in silico evaluation of a new series of oxadiazole-based anticancer agents as potential Akt and FAK inhibitors. Oxadiazoles 72-82 PTK2 protein tyrosine kinase 2 Mus musculus 128-131 29864929-0 2018 Synthesis and amelioration of inflammatory paw edema by novel benzophenone appended oxadiazole derivatives by exhibiting cyclooxygenase-2 antagonist activity. Oxadiazoles 84-94 prostaglandin-endoperoxide synthase 2 Homo sapiens 121-137 28677624-0 2017 Synthesis and Evaluation of New Oxadiazole, Thiadiazole, and Triazole Derivatives as Potential Anticancer Agents Targeting MMP-9. Oxadiazoles 32-42 matrix metallopeptidase 9 Mus musculus 123-128 27928588-3 2017 In this study, the binding modes and inhibition mechanisms of the new oxadiazole-based amide inhibitors of the human soluble epoxide hydrolase were investigated by molecular docking and molecular dynamics (MD) simulation followed by the MM-GBSA method to calculate the binding free energy of each inhibitor to sEH. Oxadiazoles 70-80 epoxide hydrolase 2 Homo sapiens 117-142 27928588-3 2017 In this study, the binding modes and inhibition mechanisms of the new oxadiazole-based amide inhibitors of the human soluble epoxide hydrolase were investigated by molecular docking and molecular dynamics (MD) simulation followed by the MM-GBSA method to calculate the binding free energy of each inhibitor to sEH. Oxadiazoles 70-80 epoxide hydrolase 2 Homo sapiens 310-313 28067996-3 2017 Further study of the structure-activity relationship of the most active compound of the first series, compound 1, led to the discovery of a novel oxadiazole analogue, compound 16j, that was a more potent small-molecule inhibitor of Bcl-2. Oxadiazoles 146-156 BCL2 apoptosis regulator Homo sapiens 232-237 29050220-6 2017 With the aid of computer modeling for screening of chemicals targeting activation function 2 (AF-2) of AR, we identified oxadiazole derivatives as good candidates and subsequently generated a small library of these compounds. Oxadiazoles 121-131 androgen receptor Homo sapiens 103-105 27544072-1 2016 In continuation of our previous efforts directed towards the development of potent and selective inhibitors of aldose reductase (ALR2), and to control the diabetes mellitus (DM), a chronic metabolic disease, we synthesized novel coumarin-thiazole 6(a-o) and coumarin-oxadiazole 11(a-h) hybrids and screened for their inhibitory activity against aldose reductase (ALR2), for the selectivity against aldehyde reductase (ALR1). Oxadiazoles 267-277 aldo-keto reductase family 1 member B Homo sapiens 129-133 27544072-9 2016 Hence, the results of this study revealed that coumarinyl thiazole and oxadiazole derivatives could act as potential ALR1/ALR2 inhibitors. Oxadiazoles 71-81 aldo-keto reductase family 1 member B Homo sapiens 122-126 28160943-0 2017 Synthesis and in silico studies of novel sulfonamides having oxadiazole ring: As beta-glucuronidase inhibitors. Oxadiazoles 61-71 glucuronidase beta Homo sapiens 81-99 27923497-6 2017 Molecular docking study showed that morpholine and oxadiazole rings linked to the benzimidazole nucleus play an important role in binding with the COX-2. Oxadiazoles 51-61 cytochrome c oxidase II, mitochondrial Rattus norvegicus 147-152 27987485-0 2017 Design, synthesis, docking and QSAR study of substituted benzimidazole linked oxadiazole as cytotoxic agents, EGFR and erbB2 receptor inhibitors. Oxadiazoles 78-88 epidermal growth factor receptor Homo sapiens 110-114 27987485-0 2017 Design, synthesis, docking and QSAR study of substituted benzimidazole linked oxadiazole as cytotoxic agents, EGFR and erbB2 receptor inhibitors. Oxadiazoles 78-88 erb-b2 receptor tyrosine kinase 2 Homo sapiens 119-124 27987485-1 2017 The synthesis of benzimidazole linked oxadiazole derivatives designed as potential EGFR and erbB2 receptor inhibitors with anticancer and apoptotic activity were studied. Oxadiazoles 38-48 epidermal growth factor receptor Homo sapiens 83-87 27987485-1 2017 The synthesis of benzimidazole linked oxadiazole derivatives designed as potential EGFR and erbB2 receptor inhibitors with anticancer and apoptotic activity were studied. Oxadiazoles 38-48 erb-b2 receptor tyrosine kinase 2 Homo sapiens 92-97