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Bioorg Med Chem Lett ; 11(7): 879-82, 2001 Apr 09.
Article in English | MEDLINE | ID: mdl-11294382

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.


Subject(s)
Gout Suppressants/chemical synthesis , Gout Suppressants/pharmacology , Pyrazoles/chemical synthesis , Pyrazoles/pharmacology , Uric Acid/antagonists & inhibitors , Uric Acid/blood , Xanthine Oxidase/antagonists & inhibitors , Allopurinol/pharmacology , Animals , Area Under Curve , Gout/drug therapy , Gout Suppressants/metabolism , Male , Metabolic Diseases/chemically induced , Metabolic Diseases/drug therapy , Models, Animal , Pyrazoles/metabolism , Rats , Rats, Sprague-Dawley , Structure-Activity Relationship , Urate Oxidase/antagonists & inhibitors , Urate Oxidase/metabolism , Uric Acid/metabolism , Xanthine Oxidase/metabolism
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