Discovery of (3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic acid (PF-3882845), an orally efficacious mineralocorticoid receptor (MR) antagonist for hypertension and nephropathy.
第一作者:
Marvin J,Meyers
第一单位:
St. Louis Laboratories, Pfizer Global Research and Development, Pfizer, Inc., 700 Chesterfield Parkway West, Chesterfield, Missouri 63017, USA. mmeyers8@slu.edu
作者:
医学主题词
动物(Animals);抗高血压药(Antihypertensive Agents);血压(Blood Pressure);细胞系, 肿瘤(Cell Line, Tumor);氯苯类(Chlorobenzenes);结晶学, X线(Crystallography, X-Ray);人类(Humans);高血压(Hypertension);吲唑类(Indazoles);茚类(Indenes);肾疾病(Kidney Diseases);男(雄)性(Male);模型, 分子(Models, Molecular);分子构象(Molecular Conformation);腈类(Nitriles);放射配体测定(Radioligand Assay);大鼠(Rats);大鼠, 近交Dahl(Rats, Inbred Dahl);大鼠, Sprague-Dawley(Rats, Sprague-Dawley);立体异构现象(Stereoisomerism);构效关系(Structure-Activity Relationship)
DOI
10.1021/jm100505n
PMID
20672822
发布时间
2021-12-03
- 浏览88
Journal of medicinal chemistry
5979-6002页
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