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.
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页码：1459 / 1465
页数：7
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