Synthesis of novel 2-mercaptobenzoxazole based 1,2,3-triazoles as inhibitors of proinflammatory cytokines and suppressors of COX-2 gene expression

摘要: A library of novel bis-heterocycles containing 2-mercaptobenzoxazole based 1,2,3-triazoles has been synthesized using click chemistry approach. The compound 4 exhibited the most potent in vivo anti-inflammatory activity with 66.66% and 61.11% inhibition in comparison to celecoxib which showed 72.22% 65.55% after 3 h 5 h respectively. compounds 9 suppressed COX-2 gene expression by 0.94 0.79 fold a selective index (COX-1/COX-2) 64.79 66.47 respectively (SI value 75.56). silico molecular docking studies interactions these molecules Tyr-59, Tyr-119 Gly-121. When compared standard drug celecoxib, 4, 5, 7, 16 did not cause any gastric ulceration.