Design, synthesis and biological evaluation of benzoxazole derivatives as cyclooxygenase inhibitors
By Srinivas Ampati, Vidya Sagar Jenugu, Raju Jukanti, Rama Ganta and 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.
Key words: Benzaxozoles, synthesis, cyclooxygenase, evaluation, COX-2, COX-1.