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Design, synthesis and bioactivities of Celecoxib analogues or derivatives
Shiyang Zhou1, Shanbin Yang1, Gangliang Huang1
1College of Chemistry, Chongqing Normal University, Chongqing 401331, China; University Bioactive Substance Engineering Research Center in Chongqing, Chongqing Normal University, Chongqing 401331, China.
Abstract:
A series of Celecoxib analogues or derivatives were designed and synthesized, and their biological activities were studied. The results of inhibitory activity in vitro proved that compounds 1a, 1h, 1i, 1l and 1p had better inhibitory effect on COX-2, and the selectivity was higher. Among them, the inhibitory activity of compound 1h to COX-2 was IC50=0.049μmol/L and SI >1000. Moreover, the experimental results of anti-inflammatory activity in vivo showed that they had good anti-inflammatory activity and could inhibit the release of PGE-2. Therefore, these compounds have better druggability.
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