QUINAZOLINONES-2 - QSAR AND INVIVO CHARACTERIZATION OF AT1 SELECTIVE AII ANTAGONISTS

被引：18

作者：

DELASZLO, SE

ALLEN, EE

QUAGLIATO, CS

GREENLEE, WJ

PATCHETT, AA

NACHBAR, RB

SIEGL, PKS

CHANG, RS

KIVLIGHN, SD

SCHORN, TS

FAUST, KA

CHEN, TB

ZINGARO, GJ

LOTTI, VJ

机构：

[1] MERCK SHARP & DOHME LTD,DEPT MOLEC SYST,RAHWAY,NJ 07065

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1993年 / 3卷 / 06期

关键词：

D O I：

10.1016/S0960-894X(00)80335-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The structure activity relationship, linear regression analysis and in vivo evaluation of a series of substituted 2-butyl-3-[(2'-tetrazol-5-yl)biphen-4-yl)methyl]quinazolin-4(1H)-ones as antagonists of the AT1 receptor for angiotensin II is presented. L-159,093 (2-butyl-6-(N-isopropyl-N-methyl-carbamoyl)amino-3-[(2'-tetrazol-5-yl)biphen-4-yl)methyl]quin azolin-4(1H)-one (IC50=0.1 nM rabbit aorta) is shown to be a potent orally active AII antagonist in rats and rhesus.

引用

页码：1299 / 1304

页数：6

共 11 条

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