Methanesulfonamide group at position-4 of the C-5-phenyl ring of 1,5-diarylpyrazole affords a potent class of cyclooxygenase-2 (COX-2) inhibitors.

Article Details

Citation

Singh SK, Vobbalareddy S, Shivaramakrishna S, Krishnamraju A, Rajjak SA, Casturi SR, Akhila V, Rao YK

Methanesulfonamide group at position-4 of the C-5-phenyl ring of 1,5-diarylpyrazole affords a potent class of cyclooxygenase-2 (COX-2) inhibitors.

Bioorg Med Chem Lett. 2004 Apr 5;14(7):1683-8.

PubMed ID
15026050 [ View in PubMed
]
Abstract

The effect of methanesulfonamide (MeSO(2)NH) group on COX-2 inhibitory activity of 1,5-diarylpyrazole is described. While this group being at position-4 of the N(1)-phenyl ring was found to be ineffective, its installation at position-4 of the C-5 phenyl ring offered several potent and selective inhibitors of COX-2 with IC(50) as low as 30 nM.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
CelecoxibProstaglandin G/H synthase 2IC 50 (nM)36N/AN/ADetails
IndomethacinProstaglandin G/H synthase 2IC 50 (nM)7810N/AN/ADetails