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Synthesis and in-silico studies of some diaryltriazole derivatives as potential cyclooxygenase inhibitors
Journal article   Peer reviewed

Synthesis and in-silico studies of some diaryltriazole derivatives as potential cyclooxygenase inhibitors

Awwad A Radwan and Kamal E H elTahir
Archives of pharmacal research, Vol.36(5), pp.553-563
01/05/2013
DOI: https://doi.org/10.1007/s12272-013-0078-6
PMID: 23479193

Abstract

Animals Cyclooxygenase 1 - metabolism Cyclooxygenase 2 - metabolism Cyclooxygenase Inhibitors - chemical synthesis Cyclooxygenase Inhibitors - chemistry Cyclooxygenase Inhibitors - pharmacology Disease Models, Animal Edema - drug therapy Edema - enzymology Male Models, Molecular Molecular Docking Simulation Rats Rats, Sprague-Dawley Triazoles - chemical synthesis Triazoles - chemistry Triazoles - pharmacology
The synthesis of several 4-phenyl-5-pyridin-4-yl-2,3-dihydro-3H-1,2,4-triazole-3-thiones possessing N-2 Mannich bases or S-alkyl substituents, is reported. Several of them exhibited a low nanomolar COX enzyme inhibition activity. Most of the compounds showed inhibition of edema was similar to that evoked by celocoxib in animal model. Molecular docking studies of the compounds into the binding sites of COX-1 and COX-2 allowed us to shed light on the binding mode of these novel COX inhibitors.

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