4-(4-Phenylsubstituted)-1,2,3-triazolacetic acid derivatives in vitro inhibitors of prostaglandin synthesis

Farmaco Sci. 1985 Feb;40(2):73-85. doi: 10.1002/chin.198530217.

Abstract

New 4-(4-phenylsubstituted)-1,2,3-triazolacetic acid derivatives of general formula (I) were prepared by nucleophilic substitution, 1,3-dipolar cycloaddition and functional group interconversion reactions. These compounds were evaluated as in vitro prostaglandin synthesis inhibitors. Only the isomeric compounds (II c) and (III e), with a 4-aminophenyl substituent on the triazole ring, inhibit arachidonic acid-induced malondialdehyde formation in human platelets; (II c) and (III e) are as effective as aspirin.

MeSH terms

  • Anti-Inflammatory Agents / chemical synthesis
  • Cyclooxygenase Inhibitors
  • Humans
  • In Vitro Techniques
  • Isomerism
  • Lipid Metabolism
  • Magnetic Resonance Spectroscopy
  • Prostaglandin Antagonists / chemical synthesis*
  • Structure-Activity Relationship
  • Triazoles / chemical synthesis*
  • Triazoles / pharmacology

Substances

  • Anti-Inflammatory Agents
  • Cyclooxygenase Inhibitors
  • Prostaglandin Antagonists
  • Triazoles