Synthesis and cardiovascular activity of phenylalkylamine derivatives. I. Potential specific bradycardic agents.
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/dtmax or mean aortic pressure in anesthetized dogs.
Ozaki
F
F
Eisai Tsukuba Research Laboratories, Ibaraki, Japan.
Matsukura
M
M
Kabasawa
Y
Y
Ishibashi
K
K
Ikemori
M
M
Hamano
S
S
Minami
N
N
D000818:Animals; D001919:Bradycardia / Q000139:chemically induced*; D002316:Cardiotonic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D004285:Dogs; D005260:Female; D006168:Guinea Pigs; D008297:Male; D014700:Verapamil / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*
D002316:Cardiotonic Agents; D014700:Verapamil