QUINAZOLINONE BIPHENYL ACYLSULFONAMIDES - A POTENT NEW CLASS OF ANGIOTENSIN-II RECEPTOR ANTAGONISTS

被引：16

作者：

CHAKRAVARTY, PK ^{[1
]}

STRELITZ, RA ^{[1
]}

CHEN, TB ^{[1
]}

CHANG, RSL ^{[1
]}

LOTTI, VJ ^{[1
]}

ZINGARO, GJ ^{[1
]}

SCHORN, TW ^{[1
]}

KIVLIGHN, SD ^{[1
]}

SIEGL, PKS ^{[1
]}

PATCHETT, AA ^{[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)81125-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new series of quinazolinone-based AT(1) selective antagonists, bearing acylsulfonamides (-SO(2)NHCOR) as the tetrazole bioisosteres, was evaluated. While AT(1) potencies remained similar to the tetrazole analogs, the AT(2) receptor affinities were significantly improved with the introduction of acylsulfonamide groups. Several of these antagonists displayed improved in vivo properties.

引用

页码：75 / 80

页数：6

共 26 条

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