4-(4-Phenylsubstituted)-1,2,3-triazolacetic acid derivatives in vitro inhibitors of prostaglandin synthesis.
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.
D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis; D016861:Cyclooxygenase Inhibitors; D006801:Humans; D066298:In Vitro Techniques; D007536:Isomerism; D050356:Lipid Metabolism; D009682:Magnetic Resonance Spectroscopy; D011448:Prostaglandin Antagonists / Q000138:chemical synthesis*; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology
D000893:Anti-Inflammatory Agents; D016861:Cyclooxygenase Inhibitors; D011448:Prostaglandin Antagonists; D014230:Triazoles