联苯八元氧桥环新烟碱增效剂的设计、合成及其增效活性  

Design,synthesis,and synergistic activity of biphenyl eight-membered oxabridge neonicotinoid analogues

作　　者：王轶平 须志平[1] 徐晓勇[1] 李忠[1] WANG Yiping;XU Zhiping;XU Xiaoyong;LI Zhong(Shanghai Key Laboratory of Chemical Biology,School of Pharmacy,East China University of Science and Technology,Shanghai 200237,China)

机构地区：[1]上海市化学生物学重点实验室,华东理工大学药学院,上海200237

出　　处：《农药学学报》2023年第6期1238-1249,共12页Chinese Journal of Pesticide Science

基　　金：国家重点研发计划(2017YFD0200500)。

摘　　要：新烟碱杀虫剂作为一类重要的杀虫剂广泛应用于刺吸式口器害虫的防治。随着应用范围的扩大和应用时间的延长,新烟碱杀虫剂的抗性水平逐渐增加,其药效减弱。本文在前期研究的基础上,开发了一类联苯八元氧桥环新烟碱类似物,以苜蓿蚜Aphis Craccivora为测试靶标测试了目标化合物与新烟碱杀虫剂代表化合物吡虫啉联用时的增效作用,测试结果表明,目标化合物对吡虫啉有一定的增效作用。其中化合物D3在1 mg/L的联用浓度下对吡虫啉的增效倍数可达4.04倍,显著增加了吡虫啉对苜蓿蚜的杀虫活性,对解决传统新烟碱杀虫剂面临的抗性问题具有重要意义。Neonicotinoids have been widely used as an important class of insecticides for controlling sap-feeding insects.However,increasing application scope and duration have led to the development of neonicotinoid resistance,decreasing their efficacy.In this study,a series of biphenyl eight-membered oxabridge neonicotinoid analogues were developed based on our previous work.The synergistic activities of target compounds in combination with imidacloprid against the cowpea aphid(Aphis Craccivora)were evaluated,and the results showed that they could effectively enhance the insecticide activities of imidacloprid against A.Craccivora.Notably,compound D3 exhibited obvious synergistic action,causing a 4.04-fold increase in the insecticide activity of imidacloprid against A.Craccivora at a combination concentration of 1 mg/L.This work holds great significance for addressing the resistance issues faced by traditional neonicotinoids.

关 键 词：新烟碱杀虫剂 联苯八元氧桥环新烟碱类似物 吡虫啉 增效剂 增效作用 

分 类 号：TQ453.2[化学工程—农药化工]