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.
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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
Drug Target Property Measurement pH Temperature (°C) Celecoxib Prostaglandin G/H synthase 2 IC 50 (nM) 36 N/A N/A Details Indomethacin Prostaglandin G/H synthase 2 IC 50 (nM) 7810 N/A N/A Details