SPECIFIC BRADYCARDIC AGENTS .2. HETEROAROMATIC MODIFICATIONS IN THE SIDE-CHAIN OF SPECIFIC BRADYCARDIC BENZAZEPINONES - CHEMISTRY, PHARMACOLOGY, AND STRUCTURE-ACTIVITY-RELATIONSHIPS

被引：19

作者：

BOMHARD, A ^{[1
]}

REIFFEN, M ^{[1
]}

HEIDER, J ^{[1
]}

PSIORZ, M ^{[1
]}

LILLIE, C ^{[1
]}

机构：

[1] ERNST BOEHRINGER INST ARZNEIMITTELFORSCH,DEPT PHARMACOL,A-1121 VIENNA,AUSTRIA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1991年 / 34卷 / 03期

关键词：

D O I：

10.1021/jm00107a011

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Compound 1 (UL-FS 49) has recently been described as the representative of a novel class of antischemic compounds termed ''specific bradycardic agents''. In search of specific bradycardic agents with different pharmacokinetic profiles, heteroaromatic analogues of 1 have been synthesized and evaluated for their bradycardic activity, selectivity, and duration of action. The chain length n and the nature of the heteroaromatic system of compounds 2 strongly determine the biological activities. Unsubstituted benzothiophenes and benzofurans in combination with a chain length of n = 2 give the most active bradycardic compounds. Some of the new compounds combine high bradycardic potency and selectivity with a short duration of action and may thus be useful for the development of short-acting specific bradycardic drugs.

引用

页码：942 / 947

页数：6

共 20 条

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