Abstract
The introduction of a hydroxyl group into the 5-position of the diaryl furanone system provides highly selective inhibitors of cyclooxygenase-2. These molecules can be converted into their sodium salts which are water soluble, facilitating intravenous formulation. These salts show excellent potency in rat models of pain, fever and inflammation.
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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Arthritis, Experimental / drug therapy
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CHO Cells
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Chemical Phenomena
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Chemistry, Physical
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Cricetinae
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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 / prevention & control
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Fever / chemically induced
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Fever / drug therapy
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Furans / chemical synthesis*
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Furans / pharmacology*
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Humans
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Isoenzymes / metabolism*
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Membrane Proteins
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Pain / chemically induced
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Pain / drug therapy
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Prostaglandin-Endoperoxide Synthases / metabolism*
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Rats
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Solubility
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Structure-Activity Relationship
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Substrate Specificity
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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Furans
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Isoenzymes
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Membrane Proteins
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Cyclooxygenase 2
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PTGS2 protein, human
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Prostaglandin-Endoperoxide Synthases