TRIAZOLINONES AS NONPEPTIDE ANGIOTENSIN-II ANTAGONISTS .2. DISCOVERY OF A POTENT AND ORALLY-ACTIVE TRIAZOLINONE ACYLSULFONAMIDE

被引：18

作者：

CHANG, LL ^{[1
]}

ASHTON, WT ^{[1
]}

FLANAGAN, KL ^{[1
]}

NAYLOR, EM ^{[1
]}

CHAKRAVARTY, PK ^{[1
]}

PATCHETT, AA ^{[1
]}

GREENLEE, WJ ^{[1
]}

BENDESKY, RJ ^{[1
]}

CHEN, TB ^{[1
]}

FAUST, KA ^{[1
]}

KLING, PJ ^{[1
]}

SCHAFFER, LW ^{[1
]}

SCHORN, TW ^{[1
]}

ZINGARO, GJ ^{[1
]}

CHANG, RSL ^{[1
]}

LOTTI, VJ ^{[1
]}

KIVLIGHN, SD ^{[1
]}

SIEGL, PKS ^{[1
]}

机构：

[1] MERCK SHARP & DOHME LTD, W POINT, PA 19486 USA

来源：

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

关键词：

D O I：

10.1016/S0960-894X(01)81132-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of trisubstituted triazolinones with a [2'-(N-acylsulfamoyl)biphenyl-4-yl]methyl side chain at N-4 has been prepared. The inhibition of AII presser responses by these potent AT(1)-selective An antagonists indicated some of them to be superior in vivo to their tetrazole counterparts. At 1 mg/kg, 3d (L-159,913) was effective orally with >4 h duration in dogs and had significant efficacy with >10 h duration i.v. in chimpanzees.

引用

页码：115 / 120

页数：6

共 24 条

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