小麦锈病活体筛选方法的规范化.DOCVIP

新型缬氨酸酰胺类杀菌剂的设计、合成与杀菌活性 杜秀江b , 王志鹏b，高扬b，于淑晶b ,寇俊杰a，王红学a，边强a，李正名a,b，赵卫光a,b* （南开大学 a.农药国家工程研究中心； b.元素有机化学研究所，天津 300071） 摘要：[目的]缬氨酸酰胺类杀菌剂是羧酸酰胺类杀菌剂中的重要一类杀菌剂，具有良好的环境相容性，根据羧酸酰胺类杀菌剂的结构特点，设计合成了新型的缬氨酸酰胺类杀菌剂。[方法]羧酸酰胺类杀菌剂具有共同的作用靶标，将其中肉桂酰胺和扁桃酰胺中共同具有的二烷氧基苯活性结构片段引入到缬氨酸酰胺类杀菌剂结构当中，设计合成了一系列新型的缬氨酸酰胺类杀菌剂，研究了其杀菌活性和构效关系，并进行了田间药效实验。[结果]结果表明，缬氨酸酰胺类杀菌剂引入二烷氧基苯结构片段后，部分化合物的杀菌活性优于商品化药剂异丙菌胺和烯酰吗啉，个别化合物的离体杀菌活性与双炔酰菌胺相当。[结论]新型缬氨酸酰胺类杀菌剂具有进一步开发成商品药的前景。 关键词： 缬氨酸酰胺；杀菌剂；卵菌纲；合成 Design, synthesis, and fungicidal activity of novel carboxylic acid amides DU Xiu-jiangb, WANG Zhi-pengb, GAO Yangb, YU Shu-jingb , KOU Jun-jiea, WANG Hong-xuea, BIAN Qianga, LI Zheng-minga,b , ZHAO Wei-guanga,b* （Nankai University, a. National Pesticide Engineering Research Center Abstract: [Aims] Carboxylic Acid Amide (CAA) fungicides are an important class of agricultural fungicide with oomycete activity and low toxicity toward mammalian cells. [Methods] To find CAA analogues with high activity against resistant pathogens, a series of substituted N-benzhydryl valinamide carbamate derivatives were designed and synthesized by introducing substituted aromatic rings into valinamide carbamate leads. Bioassays showed that some title compounds exhibited very good in vitro fungicidal activity against Phytophthora capsici and in vivo fungicidal activities against Pseudoperonospora cubensis. CoMFA and topomer CoMFA were performed to explore the structure–activity relationship on the basis of the in vitro data. [Results] The dimethoxy substituted aromatic analogue was found to display higher in vitro fungicidal activities against Phytophthora capsici and higher in vivo fungicidal activity against Pseudoperonospora cubensis than dimethomorph and iprovalicarb. [Conclusions] Further studies are currently underway in our laboratory to conduct field trials. Key words：Valinamide carbamates; Fungicidal activity; Oomycetes; Synthesis 基金项目：国家自然科学基金, 国家“”973“计划(2010CB126105),“十二五”国家科技支撑计划(2011BAE06B05)资助项目。