Synthesis and biological evaluation of new 1,4‐benzothiazine derivatives as potential COX‐2 inhibitors

Abstract

AbstractA series of new 2H‐benzo[1,4]thiazine derivatives were synthesized from aroylmethylidene malonates and o‐aminothiophenols by condensation/cyclization methodology in order to evaluate their COX‐2 inhibitory activity. In‐silico studies indicated that among the synthesized compounds, 5i could serve as a potential candidate for the task. So, compound 5i was taken as a model ligand for in vitro studies. The favorable outcome of the studies showed that compound 5i is indeed an excellent inhibitor of COX‐2.