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

…, P Misra, SA Rajjak, YK Rao, A Venkateswarlu

Index: Singh, Sunil K.; Reddy, P. Ganapati; Rao, K. Srinivasa; Lohray, Braj B.; Misra; Rajjak, Shaikh A.; Rao, Yeleswarapu K.; Venkateswarlu Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 2 p. 499 - 504

Full Text: HTML

Citation Number: 108

Abstract

Several chemical modifications in the N1-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.