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The following term was not found in PubMed: -dimethyl-BLAHone
Page 1
3-((R)-4-(((R)-6-(2-Bromo-4-fluorophenyl)-5-(ethoxycarbonyl)-2-(thiazol-2-yl)-3,6-dihydropyrimidin-4-yl)methyl)morpholin-2-yl)propanoic Acid (HEC72702), a Novel Hepatitis B Virus Capsid Inhibitor Based on Clinical Candidate GLS4.
Ren Q, Liu X, Yan G, Nie B, Zou Z, Li J, Chen Y, Wei Y, Huang J, Luo Z, Gu B, Goldmann S, Zhang J, Zhang Y. Ren Q, et al. J Med Chem. 2018 Feb 8;61(3):1355-1374. doi: 10.1021/acs.jmedchem.7b01914. Epub 2018 Jan 30. J Med Chem. 2018. PMID: 29381358
Effects of substitution on 9-(3-bromo-4-fluorophenyl)-5,9-dihydro-3H,4H-2,6-dioxa-4- azacyclopenta[b]naphthalene-1,8-dione, a dihydropyridine ATP-sensitive potassium channel opener.
Altenbach RJ, Brune ME, Buckner SA, Coghlan MJ, Daza AV, Fabiyi A, Gopalakrishnan M, Henry RF, Khilevich A, Kort ME, Milicic I, Scott VE, Smith JC, Whiteaker KL, Carroll WA. Altenbach RJ, et al. J Med Chem. 2006 Nov 16;49(23):6869-87. doi: 10.1021/jm060549u. J Med Chem. 2006. PMID: 17154517
Structure-activity relationships were investigated on the tricyclic dihydropyridine (DHP) KATP openers 9-(3-bromo-4-fluorophenyl)-5,9-dihydro-3H,4H-2,6-dioxa-4-azacyclopenta[b]naphthalene-1,8-dione (6) and 10-(3-bromo-4-fluorophenyl)-9,10 …
Structure-activity relationships were investigated on the tricyclic dihydropyridine (DHP) KATP openers 9-(3-bromo-4-fluorop …
(-)-(9S)-9-(3-Bromo-4-fluorophenyl)-2,3,5,6,7,9-hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide (A-278637): a novel ATP-sensitive potassium channel opener efficacious in suppressing urinary bladder contractions. I. In vitro characterization.
Gopalakrishnan M, Buckner SA, Whiteaker KL, Shieh CC, Molinari EJ, Milicic I, Daza AV, Davis-Taber R, Scott VE, Sellers D, Chess-Williams R, Chapple CR, Liu Y, Liu D, Brioni JD, Sullivan JP, Williams M, Carroll WA, Coghlan MJ. Gopalakrishnan M, et al. J Pharmacol Exp Ther. 2002 Oct;303(1):379-86. doi: 10.1124/jpet.102.034538. J Pharmacol Exp Ther. 2002. PMID: 12235274
In this study, we describe the preclinical pharmacology of (-)-(9S)-9-(3-bromo-4-fluorophenyl)-2,3,5,6,7,9-hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide (A-278637), a novel 1,4-dihydropyridine K(ATP) channel opener (KCO) that demonstrates enhanced blad …
In this study, we describe the preclinical pharmacology of (-)-(9S)-9-(3-bromo-4-fluorophenyl)-2,3,5,6,7,9-hexahydrothi …
(-)-(9S)-9-(3-Bromo-4-fluorophenyl)-2,3,5,6,7,9-hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide (A-278637): a novel ATP-sensitive potassium channel opener efficacious in suppressing urinary bladder contractions. II. in vivo characterization.
Brune ME, Fey TA, Brioni JD, Sullivan JP, Williams M, Carroll WA, Coghlan MJ, Gopalakrishnan M. Brune ME, et al. J Pharmacol Exp Ther. 2002 Oct;303(1):387-94. doi: 10.1124/jpet.102.034553. J Pharmacol Exp Ther. 2002. PMID: 12235275
In this study, we evaluated the in vivo potency and bladder selectivity of (-)-(9S)-9-(3-bromo-4-fluorophenyl)-2,3,5,6,7,9-hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide (A-278637), a novel dihydropyridine KCO, in a pig model of detrusor instability sec …
In this study, we evaluated the in vivo potency and bladder selectivity of (-)-(9S)-9-(3-bromo-4-fluorophenyl)-2,3,5,6, …
Synthesis and structure-activity relationships of a novel series of 2,3,5,6,7,9-hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide K(ATP) channel openers: discovery of (-)-(9S)-9-(3-bromo-4-fluorophenyl)-2,3,5,6,7,9- hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide (A-278637), a potent K(ATP) opener that selectively inhibits spontaneous bladder contractions.
Carroll WA, Altenbach RJ, Bai H, Brioni JD, Brune ME, Buckner SA, Cassidy C, Chen Y, Coghlan MJ, Daza AV, Drizin I, Fey TA, Fitzgerald M, Gopalakrishnan M, Gregg RJ, Henry RF, Holladay MW, King LL, Kort ME, Kym PR, Milicic I, Tang R, Turner SC, Whiteaker KL, Yi L, Zhang H, Sullivan JP. Carroll WA, et al. J Med Chem. 2004 Jun 3;47(12):3163-79. doi: 10.1021/jm030356w. J Med Chem. 2004. PMID: 15163196
Discovery of hepatitis B virus capsid assembly inhibitors leading to a heteroaryldihydropyrimidine based clinical candidate (GLS4).
Ren Q, Liu X, Luo Z, Li J, Wang C, Goldmann S, Zhang J, Zhang Y. Ren Q, et al. Bioorg Med Chem. 2017 Feb 1;25(3):1042-1056. doi: 10.1016/j.bmc.2016.12.017. Epub 2016 Dec 19. Bioorg Med Chem. 2017. PMID: 28082068
Herein we described our lead optimization studies including the synthesis, molecular docking studies and structure-activity relationship (SAR) studies of a series of novel heteroaryldihydropyrimidine (HAP) inhibitors of HBV capsid assembly inhibitors, and the discovery of a poten …
Herein we described our lead optimization studies including the synthesis, molecular docking studies and structure-activity relationship (SA …
(-)-(9S)-9-(3-Bromo-4-fluorophenyl)-2,3,5,6,7,9-hexahydrothieno[3,2-b]quinolin-8(4H)-one 1,1-dioxide (A-278637), a novel ATP-sensitive potassium channel opener: hemodynamic comparison to ZD-6169, WAY-133537, and nifedipine in the anesthetized canine.
Fryer RM, Preusser LC, Calzadilla SV, Hu Y, Xu H, Marsh KC, Cox BF, Lin CT, Gopalakrishnan M, Reinhart GA. Fryer RM, et al. J Cardiovasc Pharmacol. 2004 Aug;44(2):137-47. doi: 10.1097/00005344-200408000-00001. J Cardiovasc Pharmacol. 2004. PMID: 15243293
Antiplatelet activity of J78 (2-Chloro-3-[2'-bromo, 4'-fluoro-phenyl]-amino-8-hydroxy-1,4-naphthoquinone), an antithrombotic agent, is mediated by thromboxane (TX) A2 receptor blockade with TXA2 synthase inhibition and suppression of cytosolic Ca2+ mobilization.
Jin YR, Cho MR, Ryu CK, Chung JH, Yuk DY, Hong JT, Lee KS, Lee JJ, Lee MY, Lim Y, Yun YP. Jin YR, et al. J Pharmacol Exp Ther. 2005 Jan;312(1):214-9. doi: 10.1124/jpet.104.073718. Epub 2004 Aug 24. J Pharmacol Exp Ther. 2005. PMID: 15328379
19 results