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Bioorg Med Chem Lett. 2004 Jan 19;14(2):499-504.

Polar substitutions in the benzenesulfonamide ring of celecoxib afford a potent 1,5-diarylpyrazole class of COX-2 inhibitors.

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Discovery Chemistry, Discovery Research-Dr. Reddy's Laboratories Ltd, Bollaram Road, 500 049, Miyapur, Hyderabad, India.


Several chemical modifications in the N(1)-benzenesulfonamide ring of celecoxib are presented. The series with a hydroxymethyl group adjacent to the sulfonamide was found to be the most potent modification that yielded many compounds selectively active against COX-2 enzyme in vitro.

[Indexed for MEDLINE]

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