title: Synthesis and structure-activity relationships of 1-phenylpyrazoles as xanthine oxidase inhibitors.
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.
authors: Drug Discovery Research Laboratories, Welfide Corporation, Osaka, Japan. ishibuchi@welfide.co.jp
authors: S
authors: S
authors: Ishibuchi
authors: H
authors: H
authors: Morimoto
authors: T
authors: T
authors: Oe
authors: T
authors: T
authors: Ikebe
authors: H
authors: H
authors: Inoue
authors: A
authors: A
authors: Fukunari
authors: M
authors: M
authors: Kamezawa
authors: I
authors: I
authors: Yamada
authors: Y
authors: Y
authors: Naka
mesh_terms: D000493:Allopurinol / Q000494:pharmacology; D000818:Animals; D019540:Area Under Curve; D006073:Gout / Q000188:drug therapy; D006074:Gout Suppressants / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D008297:Male; D008659:Metabolic Diseases / Q000139:chemically induced / Q000188:drug therapy; D023421:Models, Animal; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship; D014503:Urate Oxidase / Q000037:antagonists & inhibitors / Q000378:metabolism; D014527:Uric Acid / Q000037:antagonists & inhibitors* / Q000097:blood* / Q000378:metabolism; D014969:Xanthine Oxidase / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: C433950:1-(3-cyano-4-neopentyloxyphenyl)pyrazole-4-carboxylic acid; D006074:Gout Suppressants; D011720:Pyrazoles; D014527:Uric Acid; D000493:Allopurinol; D014969:Xanthine Oxidase; D014503:Urate Oxidase