Abstract
2-Sulfonylphenyl-3-phenyl-indole derivatives have been reported to be highly potent and selective COX-2 inhibitors previously. In this paper, the regio-isomeric analogues-2-phenyl-3-sulfonylphenyl-indoles were identified as potent and selective COX-2 inhibitors. This work led to the discovery of compounds 4a and 8a possessing higher activity than Celecoxib on cellular assay.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Cyclooxygenase 1
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Cyclooxygenase 2
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Cyclooxygenase 2 Inhibitors
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Cyclooxygenase Inhibitors / chemical synthesis*
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Cyclooxygenase Inhibitors / classification
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Cyclooxygenase Inhibitors / pharmacology*
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Indoles / chemical synthesis*
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Indoles / classification
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Indoles / pharmacology*
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Isoenzymes / antagonists & inhibitors*
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Macrophages, Peritoneal / enzymology
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Male
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Membrane Proteins
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Mice
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Mice, Inbred C57BL
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Molecular Structure
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Prostaglandin-Endoperoxide Synthases
Substances
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2-phenyl-3-sulfonylphenyl-indole
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Cyclooxygenase 2 Inhibitors
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Cyclooxygenase Inhibitors
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Indoles
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Isoenzymes
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Membrane Proteins
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Cyclooxygenase 1
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Cyclooxygenase 2
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Prostaglandin-Endoperoxide Synthases
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Ptgs1 protein, mouse