Synthesis and Herbicidal Activities of N ε -Anilinocarbonyl-N α -{3-((un)- substituted phenyl)isoxazol-5-ylcarbonyl}lysine Derivatives

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 inhibitors, a series of novel N e -anilinocarbonyl-N α -{3-((un)substituted phenyl)isoxazol-5-ylcarbonyl}lysine derivatives were designed and synthesized, and their molecular structures were verified with IR, 1 H NMR, and elemental analysis. The biological activity examined in vivo demonstrated that most of the compounds exhibited mod- erate herbicidal activities. Meanwhile, the enzyme activity of one compound 8h was tested against the spin- ach D1 protease and the result showed its inhibitive effect against the enzyme.