BETA-ADRENERGIC BLOCKING-AGENTS WITH ACUTE ANTIHYPERTENSIVE ACTIVITY

被引：28

作者：

BALDWIN, JJ

ENGELHARDT, EL

HIRSCHMANN, R

LUNDELL, GF

PONTICELLO, GS

LUDDEN, CT

SWEET, CS

SCRIABINE, A

SHARE, NN

HALL, R

机构：

[1] MERCK INST THERAPEUT RES, West Point, PA 19486 USA

[2] MERCK FROSST RES LABS, POINTE CLAIRE H9R 4P8, QUEBEC, CANADA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1979年 / 22卷 / 06期

关键词：

D O I：

10.1021/jm00192a015

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Modification of the pharmacological profile of the vasodilating/.beta.-adrenergic blocking agent 2-[4-[3-(tert-butylamino)-2-hydroxypropoxy]phenyl]-4-(trifluoromethyl)imidazole (1) was studied. Introduction of selected substituents onto the imidazole ring in place of the trifluoromethyl group yielded highly cardioselective .beta.-adrenergic blocking agents. The placement of alkyl or chloro groups onto the aryl ring of 1 produced a class of compounds characterized as antihypertensive .beta.-adrenergic blocking agents. In the examples, the acute antihypertensive activity does not appear to be due to vasodilating or .beta.2-agonist properties.

引用

页码：687 / 694

页数：8

共 20 条

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