EVALUATION OF HETEROCYCLIC ACID EQUIVALENTS AS TETRAZOLE REPLACEMENTS IN IMIDAZOPYRIDINE-BASED NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONISTS

被引：22

作者：

KIM, D ^{[1
]}

MANTLO, NB ^{[1
]}

CHANG, RSL ^{[1
]}

KIVLIGHN, SD ^{[1
]}

GREENLEE, WJ ^{[1
]}

机构：

[1] MERCK SHARP & DOHME LTD,DEPT PHARMACOL,W POINT,PA 19486

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1994年 / 4卷 / 01期

关键词：

D O I：

10.1016/S0960-894X(01)81119-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of imidazo[4,5-b]pyridine-based AII antagonists incorporating heterocyclic acid equivalents, e.g., oxathiadiazoles, thiatriazoles, and dioxobenzothiadiazines, are exemplified as novel non-peptide AII receptor antagonists. The most potent antagonist in this series, L-161,177 (IC50 = 0.7 nM, rabbit aorta), bearing the oxathiadiazole, exhibited excellent in vivo profile after both iv and oral administration to conscious rats.

引用

页码：41 / 44

页数：4

共 11 条

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