Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry and Computational Chemistry

Abstract

Design, synthesis and biological evaluation of benzoxazole derivatives as cyclooxygenase inhibitors

Author(s): Srinivas Ampati, Vidya Sagar Jenugu, Raju Jukanti, Rama Ganta, Sarangapani Manda

We have synthesized a series of methyl-2-(2-(arylideneamino)thiazole-4-ylamino)benzoxazole-5- carboxylate derivatives and investigated their ability to inhibit human cyclooxygenase-2 enzyme (COX-2). The active compounds were screened for cyclooxygenase-1 (COX-1) inhibition. Compound VI 6 is 379-fold and VI 12 is more than 465 fold selective towards COX-2 compared to COX-1. Thus, this class of compounds may serve as excellent candidates for selective COX-2 inhibition.


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