项目名称: 硝基缩氨基胍类化合物的结构优化、杀虫活性及机理研究
项目编号: No.31272076
项目类型: 面上项目
立项/批准年度: 2013
项目学科: 农业科学
项目作者: 马永强
作者单位: 中国农业大学
项目金额: 75万元
中文摘要: 本课题组的前期研究发现了一类结构新颖的硝基缩氨基胍类杀虫先导化合物,其具有高效、微毒、易于合成、成本低廉并对蜜蜂安全等特点,进一步研究其结构优化、杀虫谱系、定量构效关系、蛋白分子对接模拟及与一些可能靶标受体和昆虫酶的相互作用,是一项具有创新意义的基础性研究工作。在开发该先导化合物的过程中,发现了一个新的关环反应,可以从直链硝基缩氨基胍类化合物,一步制备脱氢吡虫啉(杀虫活性大约是吡虫啉10倍)的类似物――取代1,2,4-三唑啉硝亚胺类化合物,进一步优化该方法,设计合成该新型类似物,进行广谱生物筛选、构效关系、机理研究,对于创制具有自主知识产权的绿色、高效新农药和探索植物保护新技术都具有重要意义。因此本课题拟就以上两个方面展开研究。
中文关键词: 硝基缩氨基胍;关环反应;生物活性;作用机理;
英文摘要: The early studies of our research group found a novel insecticidal lead compounds, hydrocarbylidenehydrazinecarboximidamide. It has high activity against aphis and rice plant hopper, low toxicity, ease of preparation, low cost and bee safety. Based on lead compound, this project will focus on design and synthesis, insect lineages, quantitative structure-activity relationships, protein and molecular docking simulations, and receptor interactions between insect enzymes. This is an innovative basic research work. In the course of development of the lead compounds, we discoveried a new cyclized reaction from chain hydrocarbylidenehydrazinecarboximidamide to analogues of nitrogen-doping olefin imidacloprid within 1-step reaction. The insecticidal activity of olefin imidacloprid is 10 times of imidacloprid. This project will focus on improving optimization of synthesis method, biological activity, structure-activity relationship and the mechanism. This study has complete independent intellectual property rights. It is important for discovery of new green pesticides and plant protection work in china.
英文关键词: N-nitro-2hydrocarbylidenehydrzinecarboximidamides;cyclization reaction;biological activity;mechanism action;