1,4- and 2,4-substituted-1,2,3-triazoles as potential potassium channel activators. VII

Farmaco. 2005 May;60(5):367-75. doi: 10.1016/j.farmac.2005.03.004.

Abstract

New 1,4- and 2,4-substituted 1,2,3-triazole derivatives were synthesized and tested as potential BK(Ca) channel openers, as a part of a research program, which hypothesizes a pharmacophoric structure containing the 1,2,3-triazole ring. The structure-activity relationships were studied introducing some structural changes concerning molecular geometry and the presence of a hydrogen bond donor as a primary amino group and a phenolic or alcoholic hydroxy function. The compounds were prepared by nucleophilic substitution on the 1,2,3-triazole ring and by 1,3-dipolar cycloaddition of azides to selected alkynes and to phenylacetone. The new compounds tested on rat aortic rings did not exhibit any significant vasorelaxing activity.

Publication types

  • Review

MeSH terms

  • Animals
  • Chemistry, Pharmaceutical / methods
  • Potassium Channels / agonists*
  • Structure-Activity Relationship
  • Triazoles / chemical synthesis*
  • Triazoles / chemistry
  • Triazoles / pharmacology

Substances

  • Potassium Channels
  • Triazoles