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

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

  • Bioorg Med Chem Lett. 2004 Jan 19;14(2):499-504. doi: 10.1016/j.bmcl.2003.10.027.
Sunil K Singh 1,  P Ganapati Reddy,  K Srinivasa Rao,  Braj B Lohray,  P Misra,  Shaikh A Rajjak,  Yeleswarapu K Rao,  A Venkateswarlu
Affiliations

Affiliation

  • 1 Discovery Chemistry, Discovery Research-Dr. Reddy's Laboratories Ltd, Bollaram Road, 500 049, Miyapur, Hyderabad, India. [email protected]
PMID: 14698190 DOI: 10.1016/j.bmcl.2003.10.027
Abstract

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.

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