Abstract
Pyridazinone was found to be an excellent core template for selective COX-2 inhibitors. Two potent, selective and orally active COX-2 inhibitors, which were highly efficacious in rat paw edema and rat pyresis models, have been obtained.
MeSH terms
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Animals
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Cell Line
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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 / pharmacokinetics*
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Cyclooxygenase Inhibitors / pharmacology
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Edema / drug therapy
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Humans
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Inhibitory Concentration 50
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Isoenzymes / antagonists & inhibitors*
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Membrane Proteins
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Metabolic Clearance Rate
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Prostaglandin-Endoperoxide Synthases
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Pyridazines / chemical synthesis*
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Pyridazines / pharmacokinetics
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Pyridazines / pharmacology
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Rats
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Structure-Activity Relationship
Substances
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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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Pyridazines
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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
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Ptgs1 protein, rat