SELECTIVE CLASS-III ANTIARRHYTHMIC AGENTS .1. BIS(ARYLALKYL)AMINES

被引：58

作者：

CROSS, PE ^{[1
]}

ARROWSMITH, JE ^{[1
]}

THOMAS, GN ^{[1
]}

GWILT, M ^{[1
]}

BURGES, RA ^{[1
]}

HIGGINS, AJ ^{[1
]}

机构：

[1] PFIZER LTD,DEPT BIOL,SANDWICH CT13 9NJ,KENT,ENGLAND

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1990年 / 33卷 / 04期

关键词：

D O I：

10.1021/jm00166a011

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of bis(arylalkyl)amines is described and their effects on prolonging effective refractory period in isolated cardiac tissue listed. Most compounds prolonged the cardiac action potential without significantly altering the maximum rate of depolarization and may be defined as selective class III antiarrhythmic agents. It was found that a particularly advantageous structural feature was to have a methanesulfonamido moiety on both of the aryl rings. Thus, compound 16 [1-(4-methanesulfonamidophenoxy)-2-[N-(4-methanesulfonamidophenethyl)-N-methylamine]ethane] was selected for further investigations. The compound is highly potent and selective class III agent which acts by blockade of cardiac potassium channels. © 1990, American Chemical Society. All rights reserved.

引用

页码：1151 / 1155

页数：5

共 14 条

[1] MOLECULAR NEUROBIOLOGY - A ROSETTA STONE FOR K-CHANNELS [J].