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.
MeSH terms
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Cyclooxygenase 2
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Cyclooxygenase 2 Inhibitors
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Cyclooxygenase Inhibitors / chemistry*
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Cyclooxygenase Inhibitors / pharmacology
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Humans
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Isoenzymes / antagonists & inhibitors*
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Isoenzymes / metabolism
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Membrane Proteins
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Prostaglandin-Endoperoxide Synthases / metabolism
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Pyrazoles / chemistry*
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Pyrazoles / pharmacology
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Sulfonamides / chemistry*
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Sulfonamides / pharmacology
Substances
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Cyclooxygenase 2 Inhibitors
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Cyclooxygenase Inhibitors
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Isoenzymes
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Membrane Proteins
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Pyrazoles
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Sulfonamides
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methanesulfonamide
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Cyclooxygenase 2
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PTGS2 protein, human
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Prostaglandin-Endoperoxide Synthases