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

Authors
Ling, TS Shiu, S Yang, DY
Citation
Ts. Ling et al., Design and synthesis of 3-fluoro-2-oxo-3-phenylpropionic acid derivatives as potent inhibitors of 4-hydroxyphenylpyruvate dioxygenase from pig liver, BIO MED CH, 7(7), 1999, pp. 1459-1465
Citations number
29
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY
ISSN journal
09680896 → ACNP
Volume
7
Issue
7
Year of publication
1999
Pages
1459 - 1465
Database
ISI
SICI code
0968-0896(199907)7:7<1459:DASO3A>2.0.ZU;2-#
Abstract
Several rationally designed analogs of 3-fluoro-2-oxo-3-phenylpropionic aci d were chemically synthesized, and the reactions of the hydrate form of the se compounds with 4-hydroxyphenylpyruvate dioxygenase from pig liver as inh ibitors were examined. Compounds 14a and 14b were found to be potent compet itive inhibitors of the enzyme with K-i values of 10 and 22 mu M, respectiv ely. (C) 1999 Elsevier Science Ltd. All rights reserved.