菊酸乙酯的结构修饰与改造及其活性功能研究

Ethyl chrysanthemum is an main active ingredient of the Tanacetum plant in pyrethrum, is also an important drug intermediates, especially in the field of chemical pesticide research plays an important role. Because of the very toxic to aquatic organisms, may cause long-term adverse effects in the aquatic environment. Thus modifying its structure and transformation by molecular assembly and combinatorial chemistry approach, reduce its impact on the toxicity to aquatic organisms and the environment, and expand its activity is an important function of scientific significance. Therefore, ethyl chrysanthemum is as a pilot structure in this project, the molecular assembly and combinatorial chemistry method were is applied to modification and transformation of its structure, at the same time, the thiadiazole, oxadiazole, sulfide and acylhydrazone active groups were introducted to ethyl chrysanthemum structure,a series of novel ethyl chrysanthemum derivatives containing the thiadiazole sulfide, oxadiazole sulfide and hydrazone structure was designed and synthesized, the economically important crops in Guizhou common pests diamondback moth and bacteria Sclerotinia fungus, Fusarium graminearum, Fusarium oxysporum pepper, Phytophthora infestans, Rhizoctonia solani, Botrytis cinerea bacteria to study the effect of suppressing the activity of the function, and the system of its mechanism of action study, completed projects can provide important scientific basis for economically important crop pests in Guizhou prevention agents.

菊酸乙酯是菊蒿属植物除虫菊中的一个主要活性成分，也是一个重要的药物中间体，特别是农药化学研究领域具有举足轻重的作用。由于对水生生物有极高毒性，可能对水体环境产生长期不良影响。因而通过分子组装和组合化学的方法对其结构进行修饰和改造，降低其对水生生物的毒性和环境的影响，并对其展开活性功能研究是具有重要的科学意义的。因此，本项目以菊酸乙酯为先导结构，采用分子组装和组合化学的方法对其酯基进行修饰和改造，同时将噻二唑、噁二唑、硫醚和酰腙活性基团引入到菊酸乙酯的结构中，合成一系列含的噻二唑、噁二唑硫醚和酰腙结构的新型菊酸乙酯衍生物，以对贵州重要经济作物常见害虫小菜蛾和病菌油菜菌核病菌、小麦赤霉病菌、辣椒枯萎病菌、马铃薯晚疫病菌、水稻纹枯病菌、黄瓜灰霉病菌等的抑制效果来研究其活性功能，并对其构效关系与作用机制进行系统研究，项目的完成能为贵州重要经济作物的病虫害防控药剂提供重要的科学依据。