Abstract
A series of 1-phenylpyrazoles was evaluated for inhibitory activity against xanthine oxidase in vitro. Of the compounds prepared, 1-(3-cyano-4-neopentyloxyphenyl)pyrazole-4-carboxylic acid (Y-700) had the most potent enzyme inhibition and displayed longer-lasting hypouricemic action than did allopurinol in a rat model of hyperuricemia induced by the uricase inhibitor potassium oxonate.
MeSH terms
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Allopurinol / pharmacology
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Animals
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Area Under Curve
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Gout / drug therapy
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Gout Suppressants / chemical synthesis*
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Gout Suppressants / metabolism
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Gout Suppressants / pharmacology*
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Male
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Metabolic Diseases / chemically induced
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Metabolic Diseases / drug therapy
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Models, Animal
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Pyrazoles / chemical synthesis*
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Pyrazoles / metabolism
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Pyrazoles / pharmacology*
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Rats
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Rats, Sprague-Dawley
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Structure-Activity Relationship
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Urate Oxidase / antagonists & inhibitors
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Urate Oxidase / metabolism
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Uric Acid / antagonists & inhibitors*
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Uric Acid / blood*
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Uric Acid / metabolism
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Xanthine Oxidase / antagonists & inhibitors*
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Xanthine Oxidase / metabolism
Substances
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1-(3-cyano-4-neopentyloxyphenyl)pyrazole-4-carboxylic acid
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Gout Suppressants
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Pyrazoles
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Uric Acid
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Allopurinol
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Xanthine Oxidase
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Urate Oxidase