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

Article Details

Citation

Singh SK, Reddy PG, Rao KS, Lohray BB, Misra P, Rajjak SA, Rao YK, Venkateswarlu A

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.

PubMed ID
14698190 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
CelecoxibProstaglandin G/H synthase 2IC 50 (nM)36N/AN/ADetails