Acylcyclohexanedione derivatives as potential in vivo sequential inhibitors of 4-hydroxyphenylpyruvate dioxygenase and GA(20) 3beta-hydroxylase.
Acylcyclohexanedione derivatives have been designed, synthesized, and evaluated for in vitro inhibition activity against the enzyme 4-hydroxyphenylpyruvate dioxygenase (4-HPPD). The biological data demonstrated that 7 is a potent inhibitor of 4-HPPD with an IC(50) value of 40 nM. After metabolism, compound 7 has the potential to become a potent inhibitor of a second enzyme, GA(20) 3beta-hydroxylase.
Huang
Jian-Lin
JL
Department of Chemistry, Tunghai University, 181 Taichung-Kang Road Sec. 3, Taichung 407, Taiwan.
Liu
Hun-Ge
HG
Yang
Ding-Yah
DY
D015111:4-Hydroxyphenylpyruvate Dioxygenase / Q000037:antagonists & inhibitors*; D000215:Acylation; D003512:Cyclohexanones / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D006868:Hydrolysis; D020128:Inhibitory Concentration 50; D006899:Mixed Function Oxygenases / Q000037:antagonists & inhibitors* / Q000145:classification; D010937:Plant Growth Regulators / Q000737:chemistry / Q000494:pharmacology
D003512:Cyclohexanones; D004791:Enzyme Inhibitors; D010937:Plant Growth Regulators; D006899:Mixed Function Oxygenases; D015111:4-Hydroxyphenylpyruvate Dioxygenase