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Synthesis and Hypoglycemic Activity of New Nicotinonitrile-Furan Molecular Hybrids

  • D. A. Tilchenko,
  • E. Yu. Bibik,
  • V. V. Dotsenko,
  • S. G. Krivokolysko,
  • K. A. Frolov,
  • N. A. Aksenov,
  • I. V. Aksenova

摘要

Abstract

Objective: Synthesis of some new nicotinonitrile-furan hybrids and evaluation of their hypoglycemic activity. Methods: Three-component pyridine synthesis based on tandem reactions of Knoevenagel condensationMichael addition-heterocyclization using furfural, cyanothioacetamide and Meldrum’s acid (or allyl acetoacetate) as the starting reagents. Hypoglycemic effects was studied on the model of dexamethasone-induced diabetes mellitus in rats. Results and Discussion: All four new compounds (XX–XXIII) were characterized by spectral methods and found to have remarkable hypoglycemic activity. Conclusions: Some new nicotinonitrile-furan hybrids were prepared and tested in vivo for hypoglycemic activity. The compound (XX) showed more potent hypoglycemic effect that of the reference drug metformin without pronounced hepatotoxicity.