新型苯并三嗪酮杀线虫剂先导的结构多样性衍生及作用机制初探

根结线虫的危害给全球作物造成了巨大损失。熏蒸剂溴甲烷和有机磷杀线虫剂苯线磷已禁用，杀线虫剂缺乏的问题更为突出。新型杀线虫剂的研究与开发已成为国际上农药创制的热点领域之一，发现结构新颖的杀线虫剂新先导具有重要的理论研究价值和潜在的应用前景。. 本项目基于前期发现的具有杀线虫活性的1,2,3-苯并三嗪-4-酮先导结构，进行结构多样性衍生，衍生包括连接臂变换和药效团的多样性衍生，引入天然杀线虫活性结构或内吸、稳定的杂环以及植物抗病激活剂结构等，测试其对南方根结线虫的离体和活体活性，详细考察1, 2, 3-苯并三嗪-4-酮结构多样性衍生对活性的影响，建立结构和活性之间的关系；并初步探索此类化合物可能的作用机制。本项目旨在发现高活性杀线虫剂先导化合物，为解决线虫防治难题寻找新的途径，对于新农药创制和农业重要害虫防治具有重要意义。

Root-knot nematodes（Meloidogyne spp.）cause a huge loss to the world’s crops. The fumigants and organophosphorus nematicides such as methyl bromide and fenamiphos are banned, which makes the absence of the nematicides more obvious. The research and development of nematicides has become hot-spots in the field of new pesticides innovation in the world. To find nemodicidal leading compounds with new structures and novel mode of action is significant and has potential application prospects.. Based on early research on 1,2,3--benzotriazin-4-ones leading structure with nemoticidal bioactivity, this project will further carry out structure diversity derivativation and synthesis of 1,2,3--benzotriazin-4-ones. The derivativation include the change of linker and derivativation of pharmacophore, that is, the introduction of natural nematicidal structures, stable and systemic heterocyclic structures and the plant elicitor fragment etc..The bioactivities against Meloidogyne incongnita in vivo and in vitro will be measured. The influence of 1,2,3--benzotriazin-4-ones' structure derivativation to the bioactivities will be investigated in detail, then the relationship of structure and bioactivity will be summarized. The preliminary exploration of mode of action of 1,2,3--benzotriazin-4-ones structure is also carried out. . The target of this project is to find high activities leading compounds of nematicide and to seek new approach to control nematodes, which is significant for the research of new pesticides and agricultural pest management.