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与氯沙坦相关的血管紧张素模拟物咪唑环取代基的转位

Transposition of the imidazole ring substituents of angiotensin mimetics related to Losartan.

作者信息

Smith J R, Wahhab A, Moore D, Ganter R C, Moore G J

机构信息

Department of Pharmacology and Therapeutics, Faculty of Medicine, University of Calgary, Alberta, Canada.

出版信息

Drug Des Discov. 1994 Nov;12(2):113-9.

PMID:9116166
Abstract

A series of analogues related to Losartan in which the imidazole ring substituents were transposed have been prepared. Biological evaluation, both in vitro and in vivo, demonstrated that the orientation of the imidazole ring has a subtle yet significant effect upon the potency of these analogues. This information has provided an insight into the possible mode of receptor binding of Losartan and related compounds.

摘要

已制备了一系列与氯沙坦相关的类似物,其中咪唑环取代基进行了互换。体外和体内的生物学评估表明,咪唑环的取向对这些类似物的效力有微妙但显著的影响。这一信息为深入了解氯沙坦及相关化合物的受体结合可能模式提供了线索。

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