SYNTHESIS AND CARDIOVASCULAR ACTIVITY OF PHENYLALKYLAMINE DERIVATIVES .1. POTENTIAL SPECIFIC BRADYCARDIAC AGENTS

被引：7

作者：

OZAKI, F ^{[1
]}

MATSUKURA, M ^{[1
]}

KABASAWA, Y ^{[1
]}

ISHIBASHI, K ^{[1
]}

IKEMORI, M ^{[1
]}

HAMANO, S ^{[1
]}

MINAMI, N ^{[1
]}

机构：

[1] EISAI TSUKUBA RES LABS, 5-1-3 TOKOUDAI, TSUKUBA, IBARAKI 30026, JAPAN

来源：

CHEMICAL & PHARMACEUTICAL BULLETIN | 1992年 / 40卷 / 10期

关键词：

BRADYCARDIAC ACTIVITY; ANGINA PECTORIS; STRUCTURE-ACTIVITY RELATIONSHIPS; N-(OMEGA-AMINOALKYL)-N-METHYLHOMOVERATRYLAMINE; 4-(SUBSTITUTED PHENYL)-3-BUTENOIC ACID; (E)-N-[3-[N'-[2-(3,4-DIMETHOXYPHENYL)ETHYL]-N'-METHYLAMINO]PROPYL]-4-[3,4-(METHYLENEDIOXY)PHENYL]-3-BUTENAMIDE;

D O I：

10.1248/cpb.40.2735

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of acyclic amide derivatives of N-(omega-aminoalkyl)-N-methylhomoveratrylamine was synthesized and evaluated for their bradycardic activity in isolated guinea pig right atria. Among these compounds, (E)-N-[3-[N'-[2-(3,4-dimethoxyphenyl)ethyl]-N'-methylamino]propyl]4-[3,4-(methylenedioxy)phenyl]-3-butenamide (35) was the most potent in vitro and was also found to show dose-dependent bradycardia without remarkable reduction of left ventricular dp/dt(max) or mean aortic pressure in anesthetized dogs.

引用

页码：2735 / 2740

页数：6

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