几类含呋喃环仿生农药分子结构改造及作用机理研究

项目名称： 几类含呋喃环仿生农药分子结构改造及作用机理研究

项目编号： No.31272068

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： 侯太平

作者单位： 四川大学

项目金额： 75万元

中文摘要： 从生物体中寻找高活性新颖结构农药化合物并进行结构修饰，是新农药创制的重要途径和研究热点。课题组前期在对一类天然植物源的C6－C5－C6骨架结构杀虫化合物结构改造过程中，发现用呋喃环等替代C6－C5－C6 骨架中的苯环，其活性大大提高，对虫、菌均显示了较高的生物活性。本项目的目的在于以这几类含呋喃环结构的高活性化合物为优化对象，采用分子相似性分析方法，设计、合成系列目标化合物，进行活性评价研究，特别是从细胞水平，测定探针分子对昆虫细胞、植物病原菌的抑制活性。研究活性成分对细胞的抑制与凋亡规律以及与活体活性进行比较，探索与认识该类小分子对靶标相互作用规律，建立农药分子的活体活性-昆虫细胞或植物病原菌活性-农药分子构效关系的分析与评价模型，为新农药创制研究以及高活性化合物的发现提供理论依据，促进我国新农药研究领域的发展。

中文关键词： 农药；呋喃环；合成；昆虫神经细胞；机理

英文摘要： It is important method to discover the active substances from nature products and to optimize the lead compound structure based on the bioactivity for making the new pesticide. In past several years,our research group studied the activity of daphneone analogues with C6-C5-C6 structure, The research results showed that the activity will powerful increase with phenyl ring being replaced with furan ring. This kind of compounds have been shown to be a activity both of against pests and antifungal. In this program, we plan to design and synthesize a series of compounds containing furan ring according the structure similar method. We will study the relationship between the structure and activity based on the result of bioassay, especially the inhibiting cell activity. According the molecular mechanism of interaction between active substance and target. We hope set up the model about the living activity- - activity at level of cell- - relationship between the structure and activity. The research helps us discover and make ultra-activity new pesticide.

英文关键词： Pesticide；furan ring；synthesis；insect nerve cell；mechanism