Synthesis of substituted N-(4-piperidyl)-N-(3-pyridyl)amides with antiarrhythmic activity. Note 1

Pharmazie. 2000 Dec;55(12):892-5.

Abstract

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).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aconitine
  • Aminopyridines / chemical synthesis
  • Aminopyridines / pharmacology
  • Animals
  • Anti-Arrhythmia Agents / chemical synthesis*
  • Anti-Arrhythmia Agents / pharmacology
  • Arrhythmias, Cardiac / chemically induced
  • Arrhythmias, Cardiac / prevention & control
  • Chromatography, Thin Layer
  • Female
  • Gas Chromatography-Mass Spectrometry
  • Magnetic Resonance Spectroscopy
  • Male
  • Piperidines / chemical synthesis
  • Piperidines / pharmacology
  • Rats
  • Spectrophotometry, Infrared

Substances

  • Aminopyridines
  • Anti-Arrhythmia Agents
  • Piperidines
  • Aconitine