Synthesis and bioevaluation of 1-phenyl-pyrazole-4-carboxylic acid derivatives as potent xanthine oxidoreductase inhibitors
A diverse library of 1-phenyl-pyrazole-4-carboxylic acid derivatives were synthesized and evaluated for their inhibitory potency against xanthine oxidoreductase (XOR) in vitro and vivo, and the structure-activity relationship (SAR) analyses were also pres
Li, Jing,Wu, Fangping,Liu, Xingguo,Zou, Yake,Chen, Huixiong,Li, Zheng,Zhang, Lei
p. 20 - 30
(2017/09/19)
Synthesis and structure - Activity relationships of 1-phenylpyrazoles as xanthine oxidase inhibitors
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.
1-phenylpyrazole compounds and medicinal application thereof
PCT No. PCT/JP97/03840 Sec. 371 Date Sep. 22, 1998 Sec. 102(e) Date Sep. 22, 1998 PCT Filed Oct. 22, 1997 PCT Pub. No. WO98/18765 PCT Pub. Date May 7, 19981-Phenylpyrazole compounds of the formula (1): which is exemplified by 5-amino-1-(3-cyano-4-isobutoxyphenyl)pyrazole-4-carboxylic acid, an optical isomer thereof and a pharmaceutically acceptable salt thereof. These compounds have a xanthine oxidase inhibitory activity and are useful as therapeutic agents for diseases such as hyperuricacidemia and gout.
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(2008/06/13)
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