IMIDAZO[4,5-B]PYRIDINE-BASED AT(1)/AT(2) ANGIOTENSIN-II RECEPTOR ANTAGONISTS

被引：34

作者：

MANTLO, NB

KIM, D

ONDEYKA, D

CHANG, RSL

KIVLIGHN, SD

SIEGL, PKS

GREENLEE, WJ

机构：

[1] MERCK & CO INC,MERCK SHARP & DOHME RES LABS,EXPLORATORY CHEM,RAHWAY,NJ 07065

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

[3] MERCK RES LABS,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)81115-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The structure-activity relationships of 6-amido-imidazo[4,5-b]pyridine-based angiotensin II antagonists ((V) under bar) demonstrate that high affinity for the AT(1) and AT(2) receptors is largely dependent upon the R(1) and R(4) substituents. Of this series, L-162,441 and L-162,620 exhibits subnanomolar (IC50) binding affinities to both AT(1) and AT(2) receptors and potent antihypertensive effects in animals upon oral administration.

引用

页码：17 / 22

页数：6

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