Abstract
A series of 3-heteroaryloxy4-phenyl-2-5H)-furanones were prepared and evaluated for their potency and selectivity as COX-2 inhibitors. This led to the identification of L-778,736 as a potent, orally active and selective inhibitor of the COX-2 enzyme.
MeSH terms
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Animals
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Biological Availability
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CHO Cells
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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 / pharmacokinetics
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Cyclooxygenase Inhibitors / pharmacology*
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Furans / chemical synthesis*
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Furans / pharmacokinetics
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Furans / pharmacology*
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Humans
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Isoenzymes / drug effects*
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Membrane Proteins
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Prostaglandin-Endoperoxide Synthases / drug effects*
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Pyridines / chemical synthesis
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Pyridines / pharmacokinetics
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Pyridines / pharmacology
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Rats
Substances
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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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L 778736
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Membrane Proteins
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Pyridines
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Cyclooxygenase 2
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PTGS2 protein, human
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Prostaglandin-Endoperoxide Synthases