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

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. Several modificat...

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Bibliographic Details
Published in:	Bioorganic & medicinal chemistry letters Vol. 14; no. 2; pp. 499 - 504
Main Authors:	Singh, Sunil K., Reddy, P.Ganapati, Rao, K.Srinivasa, Lohray, Braj B., Misra, P., Rajjak, Shaikh A., Rao, Yeleswarapu K., Venkateswarlu, A.
Format:	Journal Article
Language:	English
Published:	Oxford Elsevier Ltd 2004 Elsevier
Subjects:	1,5-Diarylpyrazoles Benzenesulfonamide Benzenesulfonamides Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Celecoxib COX-2 inhibitors Cyclooxygenase Inhibitors - chemistry Medical sciences Pharmacology. Drug treatments Polar substitutions Pyrazoles - chemistry Sulfonamides - chemistry COX-2 inhibitors Polar substitutions 1,5-Diarylpyrazoles Benzenesulfonamide Five membered ring Sulfonamide Enzyme Nitrogen heterocycle Cyclooxygenase 2 Benzene derivatives Enzyme inhibitor Cyclooxygenase 2 inhibitor In vitro Organic sulfide Primary alcohol Non steroidal antiinflammatory agent Structure activity relation Fluorine Organic compounds Oxidoreductases Chemical synthesis
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Summary:	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. Several modifications in the N 1-benzenesulfonamide ring of celecoxib with their in vitro COX-2 inhibitory activity are reported.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2003.10.027