NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONISTS - THE DISCOVERY OF DMP-581 AND DMP-811

被引：22

作者：

CARINI, DJ

ARDECKY, RJ

ENSINGER, CL

PRUITT, JR

WEXLER, RR

WONG, PC

HUANG, SM

AUNGST, BJ

TIMMERMANS, PBMWM

机构：

[1] The DuPont Merck Pharmaceutical Company, Experimental Station, Wilmington, DE 19880-0402

来源：

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

关键词：

D O I：

10.1016/S0960-894X(01)81123-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of 4-alkylimidazoles have been prepared. Two of these compounds, DMP 581, 4-ethyl-2-propyl-1-[[2'-(1 H-tetrazol-5-yl)biphenyl-4-yl]methyl]imidazole-5-carboxaldehyde, and DMP 811, 4-ethyl-2-propyl-1-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]imidazole-5-carboxylic acid, possess among the highes oral antihypertensive potencieso acid, possess among the highest oral antihypertensive potencies yet described for an angiotensin II antagonist. In addition, prodrugs of DMP 811 have been developed to further enhance the oral bioavailability of the parent diacid.

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页码：63 / 68

页数：6

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