Design, synthesis, and evaluation of postulated transient intermediate and substrate analogues as inhibitors of 4-hydroxyphenylpyruvate dioxygenase

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Title:	Design, synthesis, and evaluation of postulated transient intermediate and substrate analogues as inhibitors of 4-hydroxyphenylpyruvate dioxygenase
Authors:	Lin, Y.-L., Huang, J.-L., Wu, C.-S., Liu, H.-G., Yang, D.-Y.
Contributors:	Department of Chemistry, Tunghai University
Date:	2002
Issue Date:	2013-05-14T09:03:54Z (UTC)
Abstract:	An epoxybenzoquinone, 4-hydroxyphenoxypropionic acid, and 2-hydroxy-3-phenyl-3-butenoic acid derivatives have been designed, synthesized, and evaluated for in vitro inhibition activity against 4-hydroxyphenylpyruvate dioxygenase (4-HPPD) from pig liver by the spectrophotometric enol-borate method. The biological data demonstrated that neither epoxybenzoquinone ester nor 2-hydroxy-3-phenyl-3-butenoic acid is an inhibitor of 4-HPPD. The most potent 4-HPPD inhibitor tested was 3-hydroxy-4-phenyl-2(5H)-furanone with an IC 50 value of 0.5 μM, which may serve as a lead compound for further design of more potent 4-HPPD inhibitors. ? 2002 Elsevier Science Ltd. All rights reserved.
Relation:	Bioorganic and Medicinal Chemistry Letters Volume 12, Issue 13, 8 July 2002, Pages 1709-1713
Appears in Collections:	[Department of Chemistry ] Periodical Articles

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