ORALLY-ACTIVE PRODRUGS OF QUINOLINE-4-CARBOXYLIC ACID ANGIOTENSIN-II RECEPTOR ANTAGONISTS

被引：24

作者：

RYONO, DE

LLOYD, J

POSS, MA

BIRD, JE

BUOTE, J

CHONG, S

DEJNEKA, T

DICKINSON, KEJ

GU, Z

MATHERS, P

MORELAND, S

MORRISON, RA

PETRILLO, EW

POWELL, JR

SCHAEFFER, T

SPITZMILLER, ER

WHITE, RE

机构：

来源：

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

关键词：

D O I：

10.1016/S0960-894X(01)81147-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Prodrug derivatization of a potent quinoline-4-carboxylic acid angiotensin II receptor antagonist was undertaken as an approach to achieve improved oral activity. A dioxolenone carboxylic ester and an alkylated tetrazole prodrug both showed greater oral antihypertensive activity in the salt-deplete spontaneously hypertensive rat and increased oral bioavailability relative to the parent compound.

引用

页码：201 / 206

页数：6