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 IC50 value of 40nM. After metabolism, compound 7 has the potential to become a potent inhibitor of a second enzyme, GA20 3β-hydroxylase.