Relaxant effects of selected sildenafil analogues in the rat aorta

J Enzyme Inhib Med Chem. 2016;31(3):381-8. doi: 10.3109/14756366.2015.1024674. Epub 2015 Mar 23.

Abstract

A new series of sulfonamide derivatives of pyrazolo[4,3-e][1,2,4]triazine with chiral amino group has been synthesized and characterized. The compounds were tested for their relaxant effects in the rat aorta. Evaluation of prepared derivatives demonstrated that compound (8a) is probably a non-selective phosphodiesterase (PDE) inhibitor, as it induced aortic relaxation through endothelium-independent mechanism.

Keywords: PDE5 inhibitors; pyrazolo[4,3-e][1,2,4]triazine; relaxant effect; sildenafil analogues; sulfonamides.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Aorta / drug effects*
  • Aorta / physiology*
  • Cyclic Nucleotide Phosphodiesterases, Type 5 / metabolism
  • Dose-Response Relationship, Drug
  • Male
  • Molecular Structure
  • Phosphodiesterase 5 Inhibitors / chemical synthesis
  • Phosphodiesterase 5 Inhibitors / chemistry
  • Phosphodiesterase 5 Inhibitors / pharmacology*
  • Rats
  • Rats, Wistar
  • Sildenafil Citrate / analogs & derivatives*
  • Sildenafil Citrate / chemistry
  • Sildenafil Citrate / pharmacology
  • Structure-Activity Relationship
  • Vasodilation / drug effects*

Substances

  • Phosphodiesterase 5 Inhibitors
  • Sildenafil Citrate
  • Cyclic Nucleotide Phosphodiesterases, Type 5