Recently the D1 protease locating in the thylakoids of higher plants was found to be a potential herbicidal target. Based on one lead hit N^α-(isoxazol-5-ylcarbonyl)lysine of D1 protease inhibi-tors, a series of novel N^ε-anilinocarbonyl-N^α-{3-[(un)substituted phenyl]isoxazol-5-ylcarbonyl}lysine derivatives were designed and synthesized, and their molecular struc-tures were verified with IR, ¹H NMR, and elemental analysis. The biological activity examined in vivo demonstrated that most of the compounds exhibited moderate herbicidal activities. Mean-while, the enzyme activity of one compound 8h was tested against the spinach D1 protease and the result showed its inhibitive effect against the enzyme.

Key words: D1 protease, inhibitor, isoxazolecarbonyllysine derivative, synthesis, herbicide