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
