PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 15341931-0 2004 Novel pyrazinone inhibitors of mast cell tryptase: synthesis and SAR evaluation. 2-Hydroxypyrazine 6-16 tryptase delta 1 Homo sapiens 31-49 23085160-0 2012 Exploring the structure determinants of pyrazinone derivatives as PDE5 3HC8 inhibitors: an in silico analysis. 2-Hydroxypyrazine 40-50 phosphodiesterase 5A Homo sapiens 66-70 23085160-8 2012 (5) Hydrophobic forces and pi-pi stacking interaction with Phe786 and Phe820 are crucial in determining the binding of pyrazinone derivatives to PDE5. 2-Hydroxypyrazine 119-129 phosphodiesterase 5A Homo sapiens 145-149 19833844-0 2010 Comparative biotransformation of pyrazinone-containing corticotropin-releasing factor receptor-1 antagonists: minimizing the reactive metabolite formation. 2-Hydroxypyrazine 33-43 corticotropin releasing hormone receptor 1 Rattus norvegicus 55-96 19833844-10 2010 To reduce potential liability due to metabolic activation of BMS-665053, a number of pyrazinone analogs with different substituents were synthesized and investigated for reactive metabolite formation, leading to the discovery of a CRF-R1 antagonist with diminished in vitro metabolic activation. 2-Hydroxypyrazine 85-95 corticotropin releasing hormone receptor 1 Rattus norvegicus 231-237 19817410-4 2009 In addition, a pyrazinone-type Maillard product, 2-(5-(furan-2-yl)-6-methyl-2-oxopyrazin-1(2H)-yl) acetic acid (IIa), was identified as an intermediate for reaction product adduct II, whereas 3-deoxy-2-hexosulose was identified as an intermediate of adduct I. 2-Hydroxypyrazine 15-25 ATPase, class II, type 9A Mus musculus 112-115 18821254-2 2008 Recent efforts in the development and biological evaluation of small molecule inhibitors of Akt have led to the identification of novel Akt kinase inhibitors, based on a quinoxaline or pyrazinone scaffold. 2-Hydroxypyrazine 185-195 AKT serine/threonine kinase 1 Homo sapiens 92-95 18821254-2 2008 Recent efforts in the development and biological evaluation of small molecule inhibitors of Akt have led to the identification of novel Akt kinase inhibitors, based on a quinoxaline or pyrazinone scaffold. 2-Hydroxypyrazine 185-195 AKT serine/threonine kinase 1 Homo sapiens 136-139 18606544-0 2008 Pyrrolidinyl pyridone and pyrazinone analogues as potent inhibitors of prolyl oligopeptidase (POP). 2-Hydroxypyrazine 26-36 prolyl endopeptidase Homo sapiens 71-92 18606544-0 2008 Pyrrolidinyl pyridone and pyrazinone analogues as potent inhibitors of prolyl oligopeptidase (POP). 2-Hydroxypyrazine 26-36 prolyl endopeptidase Homo sapiens 94-97 16137886-1 2005 Thrombin-inhibitor X-ray crystal structures, in combination with the installation of binding elements optimized within the pyrazinone series of thrombin inhibitors, were utilized to transform a weak triazolopyrimidine lead into a series of potent oxazolopyridines. 2-Hydroxypyrazine 123-133 coagulation factor II, thrombin Homo sapiens 0-8 16137886-1 2005 Thrombin-inhibitor X-ray crystal structures, in combination with the installation of binding elements optimized within the pyrazinone series of thrombin inhibitors, were utilized to transform a weak triazolopyrimidine lead into a series of potent oxazolopyridines. 2-Hydroxypyrazine 123-133 coagulation factor II, thrombin Homo sapiens 144-152 15890436-1 2005 The design, synthesis and biological activity of new thrombin inhibitors with a pyridinone or pyrazinone core and different heterobicyclic P(1) arginine side-chain mimetics are described. 2-Hydroxypyrazine 94-104 coagulation factor II, thrombin Homo sapiens 53-61 15341931-1 2004 In this manuscript, the synthesis and SAR evaluation of a novel pyrazinone class of tryptase inhibitors is described. 2-Hydroxypyrazine 64-74 tryptase delta 1 Homo sapiens 84-92 12873514-1 2003 A series of potent and selective proline- and pyrazinone-based macrocyclic thrombin inhibitors is described. 2-Hydroxypyrazine 46-56 coagulation factor II, thrombin Homo sapiens 75-83 14604352-2 2003 A six-step preparation of thrombin inhibitor drug candidate 1 from pyrazinone 7 in 47% overall yield is described. 2-Hydroxypyrazine 67-77 coagulation factor II, thrombin Homo sapiens 26-34 12729670-1 2003 Part 6: design and synthesis of alphavbeta3 antagonists containing a pyridone or pyrazinone central scaffold. 2-Hydroxypyrazine 81-91 tankyrase 2 Homo sapiens 0-6 27020524-1 2016 A series of pyrazinone-based compounds incorporating either carbamate or aryl ether groups was synthesized and evaluated as corticotropin-releasing factor-1 (CRF1) receptor antagonists. 2-Hydroxypyrazine 12-22 corticotropin releasing hormone receptor 1 Homo sapiens 158-162 12588191-0 2003 Metabolic activation of a pyrazinone-containing thrombin inhibitor. 2-Hydroxypyrazine 26-36 coagulation factor II Rattus norvegicus 48-56 32717614-2 2020 Evaluating the structure-activity relationship of an aminoalkyl substituent at the 3 position of the 2(1H)-pyrazinone core, p38alpha potency was increased 20000-fold. 2-Hydroxypyrazine 101-117 mitogen-activated protein kinase 14 Homo sapiens 124-132 29477077-0 2018 Pan-NS3 protease inhibitors of hepatitis C virus based on an R3-elongated pyrazinone scaffold. 2-Hydroxypyrazine 74-84 KRAS proto-oncogene, GTPase Homo sapiens 4-7 29477077-1 2018 Herein, we present the design and synthesis of 2(1H)-pyrazinone based HCV NS3 protease inhibitors and show that elongated R3 urea substituents were associated with increased inhibitory potencies over several NS3 protein variants. 2-Hydroxypyrazine 47-63 KRAS proto-oncogene, GTPase Homo sapiens 74-77 29477077-1 2018 Herein, we present the design and synthesis of 2(1H)-pyrazinone based HCV NS3 protease inhibitors and show that elongated R3 urea substituents were associated with increased inhibitory potencies over several NS3 protein variants. 2-Hydroxypyrazine 47-63 KRAS proto-oncogene, GTPase Homo sapiens 208-211 27160057-0 2016 Discovery of pyrazinone based compounds that potently inhibit the drug-resistant enzyme variant R155K of the hepatitis C virus NS3 protease. 2-Hydroxypyrazine 13-23 KRAS proto-oncogene, GTPase Homo sapiens 127-130 27160057-1 2016 Herein, we present the design and synthesis of 2(1H)-pyrazinone based HCV NS3 protease inhibitors with variations in the C-terminus. 2-Hydroxypyrazine 47-63 KRAS proto-oncogene, GTPase Homo sapiens 74-77 23517538-0 2014 Achiral pyrazinone-based inhibitors of the hepatitis C virus NS3 protease and drug-resistant variants with elongated substituents directed toward the S2 pocket. 2-Hydroxypyrazine 8-18 KRAS proto-oncogene, GTPase Homo sapiens 61-64