BALANCED AT(1) AND AT(2) ANGIOTENSIN-II ANTAGONISTS .2. POTENT 5-ALPHA-HYDROXYACID IMIDAZOLYL BIPHENYL SULFONYLUREAS

被引：8

作者：

DEPREZ, P ^{[1
]}

GUILLAUME, J ^{[1
]}

CORBIER, A ^{[1
]}

FORTIN, M ^{[1
]}

VEVERT, JP ^{[1
]}

HECKMANN, B ^{[1
]}

机构：

[1] ROUSSEL UCLAF,F-93235 ROMAINVILLE,FRANCE

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 22期

关键词：

D O I：

10.1016/0960-894X(95)00479-D

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Introduction of an alpha-hydroxyacid moiety in position 5 of the imidazole ring within the imidazolyl biphenyl sulfonyl urea series significantly increased AT(2) binding. Structure activity relationship around this moiety is described and gave rise to balanced AII inhibitors with nanomolar affinity on both AT(1) and AT(2) receptors and with an AT(2)/AT(1) ratio of between 0.4 and 3.

引用

页码：2611 / 2616

页数：6

共 18 条

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