Synthesis of substituted N-(4-piperidyl)-N-(3-pyridyl)amides with antiarrhythmic activity. Note 1.
The synthesis of analogues of N,2-diphenyl-N-(4-piperidyl)acetamide endowed with antiarrhythmic activity is reported. Benzoyl, cinnamoyl, acetyl and propionyl groups replace the phenacyl group as N-acyl substituent, while pyridine replaces benzene as aromatic ring bound to the amide nitrogen. The title compounds were evaluated for antiarrhythmic activity on experimental arrhythmias induced by aconitine in rats. The presence of a n-propyl chain and an unsubstituted cinnamoyl moiety (1j) gives the highest protection against aconitine induced extrasystoles while the best efficacy against lethal effects is due to the presence of a n-propyl chain and an acetyl moiety (1m).
Pau
A
A
Dipartimento Farmaco Chimico Tossicologico, Facoltà di Farmacia, Università di Sassari, Italy.
Asproni
B
B
Boatto
G
G
Palomba
M
M
Cerri
R
R
Rimoli
M G
MG
Filippelli
W
W
Falcone
G
G
D000157:Aconitine; D000631:Aminopyridines / Q000138:chemical synthesis / Q000494:pharmacology; D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001145:Arrhythmias, Cardiac / Q000139:chemically induced / Q000517:prevention & control; D002855:Chromatography, Thin Layer; D005260:Female; D008401:Gas Chromatography-Mass Spectrometry; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D010880:Piperidines / Q000138:chemical synthesis / Q000494:pharmacology; D051381:Rats; D013055:Spectrophotometry, Infrared
D000631:Aminopyridines; D000889:Anti-Arrhythmia Agents; D010880:Piperidines; D000157:Aconitine