中文摘要：

植物细胞内囊体中的D1蛋白酶是近年来发现的潜在的除草剂作用靶标.以异噁唑甲酰赖氨酸脲先导结构信息为基础,设计合成了未见报道的异噁唑甲酰赖氨酸类化合物11个.目标化合物分子结构经IR,1HNMR,元素分析予以确证.平皿法活体生物活性测试表明部分化合物具有中等除草活性;化合物8h的离体生物活性测试表明其对D1蛋白酶有一定的抑制作用.

英文摘要：

Recently the D1 protease locating in the thylakoids of higher plants was found to be a potential herbicidal target. Based on one lead hit Nα-（isoxazol-5-ylcarbonyl）lysine of D1 protease inhibitors,a series of novel Nε-anilinocarbonyl-Nα-{3-[（un）substituted phenyl]isoxazol-5-ylcarbonyl}lysine derivatives were designed and synthesized,and their molecular structures 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. Meanwhile,the enzyme activity of one compound 8h was tested against the spinach D1 protease and the result showed its inhibitive effect against the enzyme.