Synthesis and Cardiovascular Activity of Phenylalkylamine Derivatives. I. Potential Specific Bradycardic Agents

Fumihiro OZAKI; Masayuki MATSUKURA; Yasuhiro KABASAWA; Keiji ISHIBASHI; Megumi IKEMORI; Sachiyuki HAMANO; Norio MINAMI

doi:10.1248/cpb.40.2735

著者情報

キーワード: bradycardic activity, angina pectoris, structure-activity relationships, N-(ω-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

ジャーナルフリー

1992 年 40 巻 10 号 p. 2735-2740

DOI https://doi.org/10.1248/cpb.40.2735

詳細

抄録

A series of acyclic amide derivatives of N-(ω-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.

責任著者(Corresponding author)

J-STAGEへの登録はこちら（無料）