基于化感物质Tricin设计、合成具有高选择性的生态安全除草剂

项目名称： 基于化感物质Tricin设计、合成具有高选择性的生态安全除草剂

项目编号： No.31501686

项目类型： 青年科学基金项目

立项/批准年度： 2016

项目学科： 农业科学

项目作者： 张敏

作者单位： 江苏大学

项目金额： 20万元

中文摘要： 化感物质因具有选择性强、易降解和对环境污染小的特点，为生态安全除草剂的研究提供了新思路。以化感物质Tricin(5,7,4′-三羟基-3′,5′-二甲氧基黄酮)为先导化合物进行结构优化时发现，其同分异构的橙酮类似物具有更好的除草活性和选择性。为了发现具有应用价值的橙酮类化合物，申请人采用活性片段拼接原理，将芳氧羧酸类除草剂的活性结构（芳氧乙酰基）引入到橙酮结构中，设计并合成出芳氧乙酰氧基橙酮衍生物。初步结果表明，该类化合物高选择性地抑制双子叶杂草，100g/亩时的茎叶处理效果与除草剂2,4-D相当。本项目将继续围绕芳氧乙酰氧基橙酮可修饰的位点，结合已有的构效关系，设计并合成出新的目标化合物，选择代表性的杂草作为靶标，测定其抑制种子萌发和杂草生长的活性，在此基础上进行结构与活性关系的研究，从而更进一步对目标化合物进行修饰、优化。期望通过研究找到1-2个高效、高选择性、生态安全除草剂候选品种。

中文关键词： 化感物质；设计；合成；除草活性；构效关系

英文摘要： Allelochemicals have emerged to be potentially new candidates for ecological herbicides, due to their high selectivity, easy degradability and environment-friendly characteristic. During the modification of allelochemical Tricin (5,7,4′-trihydroxy-3′,5′-dimethoxyflavone), aurones, isomers of tricins, were found to show better herbicidal activity and selectivity against dicotyledonous plants . However, when compared to the commercial herbicides, aurones show lower hericidal activity. In order to develop highly effective herbicides that are based on aurone structure, we propose that the conjunction of aryloxycarboxylic acid, a common motif found in herbicides, with aurone would produce aryloxyacetoxyaurone derivatives with higher herbicidal activity. And the preliminary bioassay results are encouraging. At the dosage of 1500 g/ha, the compounds cause 100% inhibition for dicotyledonous weeds in post-emergence treatment, equivalent to 2,4-D; moreover they showed poor effect on monocotyledons plants. In this project, the new aryloxyacetoxyaurone derivatives would be designed and synthesized based on the structure-activity relationships, and their herbicidal activities would be evaluated. Then the qualitative and quantitative structure-activity relationships will be studied, and used to guide the design of other target compounds. This research is expected to produce 1-2 highly active and selective compounds, and may lay a significant foundation for development of environment-friendly candidate herbicides or leading compounds.

英文关键词： allelochemical;design;synthesis;herbicidal activity;structure-activity relationship