A pharmacophore model for sulphonyl-urea (-cyanoguanidine) compounds with dual action, thromboxane receptor antagonists and thromboxane synthase inhibitors

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Abstract

A 3D pharmacophore model was developed for original sulphonyl-urea (-cyanoguanidine) compounds and known molecules which behave both as thromboxane receptor antagonists and as thromboxane synthase inhibitors. Five recognition sites appear to be essential for this dual activity: two hydrogen bond acceptors, an anionic site, a hydrophobic group and an aromatic ring. Such a model could be used to design new leads possessing the same pharmacological profile and to improve the activity of our compounds.

Original languageEnglish
Pages (from-to)703-710
Number of pages8
JournalEuropean Journal of Medicinal Chemistry
Volume38
Issue number7-8
DOIs
Publication statusPublished - 1 Jul 2003

Keywords

  • Catalyst hypothesis
  • Pharmacophore
  • Sulphonyl-urea (-cyanoguanidine) ligand
  • Thromboxane receptor antagonism
  • Thromboxane synthase inhibition

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