Bioorganic and Medicinal Chemistry
Bioorganic and Medicinal Chemistry
5 years ago

Design, synthesis and bioactivities of Celecoxib analogues or derivatives

Design, synthesis and bioactivities of Celecoxib analogues or derivatives
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.

Publisher URL: www.sciencedirect.com/science

DOI: S0968089617313238

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