Abstract
A new series of substituted 2-sulfonyphenyl-3-phenyl-indole derivatives were synthesized and evaluated for their ability to inhibit COX-2 and COX-1enzymes. Most of the compounds synthesized were found to be highly potent and selective inhibitors of COX-2. This work led to the discovery of 2-aminosulfonylphenyl-3-phenyl-indole 5a which possesses higher activity and selectivity for COX-2 than Celecoxib both in vitro and in vivo.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology
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Carrageenan
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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 / pharmacology*
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Edema / chemically induced
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Edema / drug therapy
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Foot / pathology
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Indicators and Reagents
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Indoles / chemical synthesis*
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Indoles / pharmacology*
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Isoenzymes / metabolism*
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Macrophages / drug effects
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Macrophages / 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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Prostaglandin-Endoperoxide Synthases / metabolism*
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Rats
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Rats, Sprague-Dawley
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Structure-Activity Relationship
Substances
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Anti-Inflammatory Agents, Non-Steroidal
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Cyclooxygenase 2 Inhibitors
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Cyclooxygenase Inhibitors
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Indicators and Reagents
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Indoles
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Isoenzymes
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Membrane Proteins
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Carrageenan
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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
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Ptgs1 protein, rat