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.
Singh
Sunil K
SK
Discovery Chemistry, Discovery Research-Dr. Reddy's Laboratories Ltd, Bollaram Road, 500 049, Miyapur, Hyderabad, India. sunilkkumarsingh@drreddys.com
Reddy
P Ganapati
PG
Rao
K Srinivasa
KS
Lohray
Braj B
BB
Misra
P
P
Rajjak
Shaikh A
SA
Rao
Yeleswarapu K
YK
Venkateswarlu
A
A
D000068579:Celecoxib; D016861:Cyclooxygenase Inhibitors / Q000737:chemistry*; D011720:Pyrazoles / Q000737:chemistry*; D013449:Sulfonamides / Q000737:chemistry*; D000096926:Benzenesulfonamides
D000068579:Celecoxib; D016861:Cyclooxygenase Inhibitors; D011720:Pyrazoles; D013449:Sulfonamides; D000096926:Benzenesulfonamides