Synthesis and antiarrhythmic activity of substituted (2-pyrimidinylthio)acetamidoximes

J Med Chem. 1975 Aug;18(8):852-4. doi: 10.1021/jm00242a021.

Abstract

A series of (2-pyrimidinylthiomethyl)carbonitriles and -carboxamidoximes was synthesized and the antiarrhythmic effects were evaluated against ventricular arrhythmias as measured by the electrical fibrillatory threshold in the anesthetized dog. Structure-activity studies indicated 2-[4-(p-chlorobenzylamino)-6-methyl-2-pyrimidinylthio]acetamidoxime dihydrochloride (6a) and 2-[4-(1,3-benzodioxol-5-ylmethylamino-6-propyl-2-pyrimidinylthio]acetamidoxime (6g) to be the most potent members of the series.

MeSH terms

  • Acetamides / chemical synthesis*
  • Acetamides / therapeutic use
  • Animals
  • Anti-Arrhythmia Agents / chemical synthesis*
  • Anti-Arrhythmia Agents / therapeutic use
  • Dogs
  • Electric Stimulation
  • Pyrimidines / chemical synthesis*
  • Pyrimidines / therapeutic use
  • Ventricular Fibrillation / prevention & control

Substances

  • Acetamides
  • Anti-Arrhythmia Agents
  • Pyrimidines