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

doi:10.1016/S0960-894X(01)00093-2

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 journal › Article › peer-review

94 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 language	English
Pages (from-to)	879-882
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	11
Issue number	7
DOIs	https://doi.org/10.1016/S0960-894X(01)00093-2
Publication status	Published - 2001 Apr 9
Externally published	Yes

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/S0960-894X(01)00093-2

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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.",

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

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T1 - Synthesis and structure - Activity relationships of 1-phenylpyrazoles as xanthine oxidase inhibitors

AU - Ishibuchi, Seigo

AU - Morimoto, Hiroshi

AU - Oe, Takanori

AU - Ikebe, Tsuguo

AU - Inoue, Hiroyoshi

AU - Fukunari, Atsushi

AU - Kamezawa, Miho

AU - Yamada, Ichimaro

AU - Naka, Yoichi

PY - 2001/4/9

Y1 - 2001/4/9

N2 - 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.

AB - 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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EP - 882

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 7

ER -

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

Abstract

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