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

Seigo Ishibuchi, Hiroshi Morimoto, Takanori Oe, Tsuguo Ikebe, Hiroyoshi Inoue, Atsushi Fukunari, Miho Kamezawa, Ichimaro Yamada, Yoichi Naka

Research output: Contribution to journalArticle

92 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)879-882
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume11
Issue number7
DOIs
Publication statusPublished - 2001 Apr 9
Externally publishedYes

Fingerprint

Xanthine Oxidase
Structure-Activity Relationship
Urate Oxidase
Enzyme inhibition
Hyperuricemia
Allopurinol
Rats
Enzymes
1-(3-cyano-4-neopentyloxyphenyl)pyrazole-4-carboxylic acid
In Vitro Techniques
potassium oxonate

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

Cite this

Synthesis and structure - Activity relationships of 1-phenylpyrazoles as xanthine oxidase inhibitors. / Ishibuchi, Seigo; Morimoto, Hiroshi; Oe, Takanori; Ikebe, Tsuguo; Inoue, Hiroyoshi; Fukunari, Atsushi; Kamezawa, Miho; Yamada, Ichimaro; Naka, Yoichi.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 11, No. 7, 09.04.2001, p. 879-882.

Research output: Contribution to journalArticle

Ishibuchi, Seigo ; Morimoto, Hiroshi ; Oe, Takanori ; Ikebe, Tsuguo ; Inoue, Hiroyoshi ; Fukunari, Atsushi ; Kamezawa, Miho ; Yamada, Ichimaro ; Naka, Yoichi. / Synthesis and structure - Activity relationships of 1-phenylpyrazoles as xanthine oxidase inhibitors. In: Bioorganic and Medicinal Chemistry Letters. 2001 ; Vol. 11, No. 7. pp. 879-882.
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