Modification of the 1,2,3-triazole ring present in an effective in vitro inhibitor of the prostaglandin synthesis

Abstract

This paper describes some modifications of the heterocyclic ring of 1-N-benzylsubstituted 1,2,3-triazoles, which are effective inhibitors of the arachidonic acid-induced malondialdehyde production in human platelets. The corresponding 1-N-imidazole- or 1-N-1,2,4-triazole-derivatives, with basic properties, preserve the inhibitory enzymatic activity, whilst the C-substituted tetrazole or 1,3,4-oxadiazole derivatives, with a neutral character, show no activity. A close structural relationship between our active compounds and Dazoxiben, a potent selective tromboxane-synthetase inhibitor, was observed.