SYNTHESIS AND ANTIHYPERTENSIVE ACTIVITY OF 4-(SUBSTITUTED-CARBONYLAMINO)-2H-1-BENZOPYRANS

被引：42

作者：

ASHWOOD, VA ^{[1
]}

CASSIDY, F ^{[1
]}

COLDWELL, MC ^{[1
]}

EVANS, JM ^{[1
]}

HAMILTON, TC ^{[1
]}

HOWLETT, DR ^{[1
]}

SMITH, DM ^{[1
]}

STEMP, G ^{[1
]}

机构：

[1] SMITHKLINE BEECHAM PHARMACEUT,MRC,HARLOW CM19 5AD,ESSEX,ENGLAND

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1990年 / 33卷 / 09期

关键词：

D O I：

10.1021/jm00171a051

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and antihypertensive activity of a series of novel 4-(substituted-carbonylamino)-2H-1-benzopyran-3-ols, administered orally to conscious spontaneously hypertensive rats, are described. Optimum activity was observed for compounds with alkyl, amino, or aryl groups flanking the carbonyl group. Of the alkyl and amino series the most potent compounds contained the methyl and methylamino groups, respectively. Several analogues have been compared with cromakalim (1) for their effects on potassium ion efflux in the rabbit mesenteric artery using rubidium-86 as a marker. The ability of each compound to enhance rubidium-86 efflux is approximately parallelled by its blood pressure lowering activity, and thus these analogues, like compound (1), belong to the series of drugs which have been classified as potassium-channel activators. © 1990, American Chemical Society. All rights reserved.

引用

页码：2667 / 2672

页数：6

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