Fine-tuning the selectivity of aldosterone synthase inhibitors: structure− activity and structure− selectivity insights from studies of heteroaryl substituted 1, 2, 5, 6- …

S Lucas, M Negri, R Heim, C Zimmer…

文献索引：Lucas, Simon; Negri, Matthias; Heim, Ralf; Zimmer, Christina; Hartmann, Rolf W. Journal of Medicinal Chemistry, 2011 , vol. 54, # 7 p. 2307 - 2319

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被引用次数: 38

摘要

Pyridine substituted 3, 4-dihydro-1 H-quinolin-2-ones (eg, 1− 3) constitute a class of highly potent and selective inhibitors of aldosterone synthase (CYP11B2), a promising target for the treatment of hyperaldosteronism, congestive heart failure, and myocardial fibrosis. Among these, ethyl-substituted 3 possesses high selectivity against CYP1A2. Rigidification of 3 by incorporation of the ethyl group into a 5-or 6-membered ring affords compounds ...