BALANCED AT(1) AND AT(2) ANGIOTENSIN-II ANTAGONISTS .1. NEW ORALLY-ACTIVE 5-CARBOXYL IMIDAZOLYL BIPHENYL SULFONYLUREAS

被引：16
作者：
DEPREZ, P
HECKMANN, B
CORBIER, A
VEVERT, JP
FORTIN, M
GUILLAUME, J
机构：
[1] Roussel Uclaf, 93235 Romainville Cedex
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 22期
关键词：
D O I：
10.1016/0960-894X(95)00478-C
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of substituted imidazolyl biphenyl sulfonylureas have been synthesized. Substitution on the imidazole ring but essentially on the urea side chain significantly increased AT(2) binding with cyclohexylmethyl, cyclopentylmethyl and benzyl as the most effective substituents. Imidazole 13d, as a representative member of this series, displayed nanomolar binding affinity for both the AT(1) and AT(2) angiotensin II receptor subtypes as well as oral activity.
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收藏
页码：2605 / 2610
页数：6
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