Design and synthesis of 3-fluoro-2-oxo-3-phenylpropionic acid derivatives as potent inhibitors of 4-hydroxyphenylpyruvate dioxygenase from pig liver

被引：8

作者：

Ling, TS ^{[1
]}

Shiu, S ^{[1
]}

Yang, DY ^{[1
]}

机构：

[1] Tunghai Univ, Dept Chem, Taichung 40704, Taiwan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 1999年 / 7卷 / 07期

关键词：

HPPD; enzyme inhibition; keto form; hydrate form;

D O I：

10.1016/S0968-0896(99)00062-0

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Several rationally designed analogs of 3-fluoro-2-oxo-3-phenylpropionic acid were chemically synthesized, and the reactions of the hydrate form of these compounds with 4-hydroxyphenylpyruvate dioxygenase from pig liver as inhibitors were examined. Compounds 14a and 14b were found to be potent competitive inhibitors of the enzyme with K-i values of 10 and 22 mu M, respectively. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

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页码：1459 / 1465

页数：7

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