Polar substitutions in the benzenesulfonamide ring of celecoxib afford a potent 1,5-diarylpyrazole class of COX-2 inhibitors.
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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
Drug Target Property Measurement pH Temperature (°C) Celecoxib Prostaglandin G/H synthase 2 IC 50 (nM) 36 N/A N/A Details