Synthesis and pharmacological evaluation of novel heterotricyclic acylhydrazone derivatives, designed as PAF antagonists

Eur J Pharm Sci. 2000 Oct;11(4):285-90. doi: 10.1016/s0928-0987(00)00102-0.

Abstract

This paper describes the synthesis and the antiplatelet properties of new heterotricyclic N-acylhydrazone derivatives (7a-e), structurally analogous to known hetrazepinic PAF antagonists, exploring molecular hybridization as a tool for molecular designing. The synthetic route employed to access compounds (7a-e) used, as starting material, the previously described methyl 3-hydroxy-8-methyl-6-phenyl-6H-pyrazolo[3,4-b]thieno[2, 3-d]pyridine-2-carboxylate derivative. The results from inhibitory effects of these novel acylhydrazone derivatives (7a-e) upon PAF-induced platelet aggregation, indicated that all compounds present a significant antithrombotic profile.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Azepines / chemistry
  • Azepines / pharmacology
  • Models, Molecular*
  • Platelet Activating Factor / antagonists & inhibitors*
  • Platelet Aggregation Inhibitors / chemistry*
  • Platelet Aggregation Inhibitors / pharmacology*
  • Rabbits
  • Triazoles / chemistry
  • Triazoles / pharmacology

Substances

  • Azepines
  • Platelet Activating Factor
  • Platelet Aggregation Inhibitors
  • Triazoles
  • bepafant