Abstract
This paper describes SAR studies involved in the transformation of the NSAID meclofenamic acid into potent and selective cyclooxygenase-2 (COX-2) inhibitors via neutralization of the carboxylate moiety in this nonselective COX inhibitor.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Amides / chemical synthesis
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Amides / chemistry
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Amides / pharmacology
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Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis
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Anti-Inflammatory Agents, Non-Steroidal / chemistry
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology
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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 / chemistry
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Cyclooxygenase Inhibitors / pharmacology
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Humans
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Inhibitory Concentration 50
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Isoenzymes / antagonists & inhibitors*
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Isoenzymes / metabolism
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Meclofenamic Acid / analogs & derivatives*
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Meclofenamic Acid / chemical synthesis
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Meclofenamic Acid / pharmacology
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Membrane Proteins
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Prostaglandin-Endoperoxide Synthases / metabolism
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Structure-Activity Relationship
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Substrate Specificity
Substances
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Amides
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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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Meclofenamic Acid
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Cyclooxygenase 1
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Cyclooxygenase 2
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PTGS1 protein, human
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PTGS2 protein, human
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Prostaglandin-Endoperoxide Synthases