Synthesis and structure-activity relationships of 1-phenylpyrazoles as xanthine oxidase inhibitors

Authors
Ishibuchi, S Morimoto, H Oe, T Ikebe, T Inoue, H Fukunari, A Kamezawa, M Yamada, I Naka, Y
Citation
S. Ishibuchi et al., Synthesis and structure-activity relationships of 1-phenylpyrazoles as xanthine oxidase inhibitors, BIOORG MED, 11(7), 2001, pp. 879-882
Citations number
9
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
7
Year of publication
2001
Pages
879 - 882
Database
ISI
SICI code
0960-894X(20010409)11:7<879:SASRO1>2.0.ZU;2-0
Abstract
A series of 1-phenylpyrazoles was evaluated for inhibitory activity against xanthine oxidase in vitro. Of the compounds prepared, 1-(3-cyano-4-neopent yloxyphenyl)pyrazole-4-carboxylic acid (Y-700) had the most potent enzyme i nhibition and displayed longer-lasting hypouricemic action than did allopur inol in a rat model of hyperuricemia induced by the uricase inhibitor potas sium oxonate. (C) 2001 Elsevier Science Ltd. All rights reserved.