Abstract
The carboxyl group of the NSAID indomethacin was replaced with a variety of substituted thiazoles to obtain a series of potent, selective inhibitors of COX-2. Additional substitutions were made at the 1-position and 5-position of the indole of indomethacin.
MeSH terms
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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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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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Humans
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Indomethacin / analogs & derivatives*
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Indomethacin / chemical synthesis
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Indomethacin / pharmacology
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Inhibitory Concentration 50
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Isoenzymes / drug effects
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Isoenzymes / metabolism*
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Membrane Proteins
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Prostaglandin-Endoperoxide Synthases / drug effects
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Prostaglandin-Endoperoxide Synthases / metabolism*
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Structure-Activity Relationship
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Thiazoles / chemical synthesis
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Thiazoles / pharmacology*
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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Isoenzymes
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Membrane Proteins
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Thiazoles
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Cyclooxygenase 2
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PTGS2 protein, human
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Prostaglandin-Endoperoxide Synthases
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Indomethacin