SYNTHESIS AND STRUCTURE-ACTIVITY-RELATIONSHIPS OF A NOVEL SERIES OF NONPEPTIDE AT(2)-SELECTIVE ANGIOTENSIN-II RECEPTOR ANTAGONISTS

被引：21

作者：

WU, MT

IKELER, TJ

ASHTON, WT

CHANG, RSL

LOTTI, VJ

GREENLEE, WJ

机构：

[1] Merch Research Laboratories, Division of Merck, Co., Inc., Rahway

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1993年 / 3卷 / 10期

关键词：

D O I：

10.1016/S0960-894X(01)81007-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of 1,4-disubstituted-piperazine-2-carboxylic acids has been discovered as AT(2)-selective non-peptide angiotensin II receptor antagonists with nanomolar or subnanomolar potency. L-159,686 [(S)-1,4-bis(N,N-diphenylcarbamoyl)piperazine-2-carboxylic acid; AT(2) IC50 1.5 nM, AT(1) IC50 > 100,000 nM] has sufficient oral bioavailability and half-life in rats for use as an in vivo pharmacological tool.

引用

页码：2023 / 2028

页数：6

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