Benzazepinone calcium channel blockers. 3. Synthesis and structure-activity studies of 3-alkylbenzazepinones

J Das, DM Floyd, SD Kimball, KJ Duff…

文献索引：Das, Jagabandhu; Floyd, David M.; Kimball, S. David; Duff, Keith J.; Vu, Truc Chi; et al. Journal of Medicinal Chemistry, 1992 , vol. 35, # 4 p. 773 - 780

全文：HTML全文

被引用次数: 26

摘要

As part of a program aimed at identifying novel analogues of diltiazem, we developed several synthetic routes for 3dkylbenzazepinones, both in racemic and nonracemic form. Structure-activity relationship studies in this series have led to identification of several analogues as potent calcium channel blocking agents, both in vitro and in vivo. Analogues containing a 6-trifluoromethyl substituent (17a and 17b) are the most potent vasorelaxants ...