Synthesis and antihyperlipaemic activity of some novel N-cyanovinylformamidines

Arzneimittelforschung. 1997 Jan;47(1):35-8.

Abstract

Potent antihyperlipaemic activity has been observed in a series of novel N-cyanovinylformamidines when tested in hyperlipaemic rats. Two of the compounds (11 and 15) were found more potent than gemfibrozil at 50 mg/kg/d dose level in reducing serum cholesterol and triglyceride levels and also in elevating serum HDL level. A good three-dimensional structural similarity has been observed between these two compounds and clofibrate and gemfibrozil, respectively. Acute toxicity studies carried out in mice indicated compound 11 to be safe even at a dose level of 4.5 g/kg. The title compounds were synthesized by the reaction of alpha-cyanoketene S,N-acetals with formamidineacetate under controlled reaction conditions.

MeSH terms

  • Animals
  • Cholesterol / blood
  • Female
  • Formamides / chemical synthesis*
  • Formamides / pharmacology
  • Formamides / toxicity
  • Gemfibrozil / pharmacology
  • Hypolipidemic Agents / chemical synthesis*
  • Hypolipidemic Agents / pharmacology
  • Hypolipidemic Agents / toxicity
  • Magnetic Resonance Spectroscopy
  • Male
  • Mice
  • Models, Molecular
  • Rats
  • Rats, Wistar
  • Spectrophotometry, Infrared
  • Triglycerides / blood

Substances

  • Formamides
  • Hypolipidemic Agents
  • Triglycerides
  • Cholesterol
  • Gemfibrozil