除草剂对保障农业稳产增收和国家粮食安全起着不可替代的作用。随着杂草抗性增加和环境保护法规的加强，应用除草剂作为作物保护手段面临巨大挑战，基于新靶标的新型除草剂创制研究成为当前的迫切需要。本项目拟以植物2C-甲基赤藓糖-4-磷酸途径（MEP途径）关键酶IspC为靶标，结合前期MEP途径关键酶IspD抑制剂先导化合物研究工作基础，以天然活性结构膦胺霉素(Fosmidomycin)、多卤代酚基吡咯(Pseudilin)、色氨酸衍生物四氢吡啶并吲哚(tetrahydropyridoindole)为核心骨架，通过引入各种含氟基团和进行前药化修饰，开展基于天然产物活性结构的含氟衍生化和前药化设计策略的除草剂发现研究。通过本项目研究内容的实现，预期发现3-5个高活性的MEP途径抑制剂化合物，对于以含氟衍生化和前药化设计策略为手段的除草活性天然产物结构优化和基于新作用模式的新型除草剂发现研究具有重要意义。

As one of the three major types of pesticides, herbicides have an irreplaceable role in achieving crop production increase and providing national food security. With the increase of weed resistance and the strengthening of environmental protection regulations, the application of herbicides as the means for crop protection faces enormous challenges, and the innovation research and development of new herbicides based on new modes of action have become a stringent need. By focusing on the key target protein IspC in the 2C-methyl-d-erythritol 4-phosphate pathway (MEP) in plants with the combination of the previous work basis on another MEP key enzyme IspD, this project will initiate the work on the rational design and synthesis of new lead compounds targeting the key enzymes in the MEP pathway. The strategies used in the molecular structural design and optimization will be the introduction of fluorine-containing functionalities and propesticide derivatization based on the core structures of herbicide-active natural products Fosmidomycin, Pseudilin, and the tryptophan-derived tetrahydropyridoindole. Through the realization of this project, it is expected to find 3-5 herbicidal lead compounds with high activity targeting the key enzymes in the MEP pathway, and the results will be of important significance toward the structural optimization of natural products and herbicide discovery of new modes of action with the strategies of fluorine-containing derivatization and proherbicide design.