- Synthesis and structure-activity relationships of 1-phenylpyrazoles as xanthine oxidase inhibitors.
Synthesis and structure-activity relationships of 1-phenylpyrazoles as xanthine oxidase inhibitors.
Bioorganic & medicinal chemistry letters (2001-04-11)
S Ishibuchi, H Morimoto, T Oe, T Ikebe, H Inoue, A Fukunari, M Kamezawa, I Yamada, Y Naka
PMID11294382
摘要
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.
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