文献类型：期刊文献

中文题名：含苄基的七元氮桥新烟碱化合物的设计、合成与杀虫活性测试

英文题名：Design, Synthesis and Insecticidal Activity of Seven-membered Azabridged Neonicotinoids Containing Benzyl Groups

作者：张凡[1];徐仁博[1];李忠[1,2];徐晓勇[1,2]

机构：[1]华东理工大学药学院上海化学生物重点实验室,上海200237;[2]中国上海生物制造技术协同创新中心,上海200237

年份：2016

卷号：55

期号：10

起止页码：715

中文期刊名：农药

外文期刊名：Agrochemicals

收录：CSTPCD;;北大核心:【北大核心2014】；CSCD:【CSCD_E2015_2016】；

基金：国家自然科学基金资助(21272071)

语种：中文

中文关键词：七元氮桥;新烟碱;杀虫剂;烟碱乙酰胆碱受体;柔性连接臂;曼尼希反应

外文关键词：seven-membered azabridge; neonicotinoids; insecticide; nAChRs; flexible linker; mannich reaction

摘要：[目的]通过在新型氮桥环新烟碱类化合物的结构中引入一个柔性连接臂(CH_2),研发新化学结构的新烟碱杀虫剂,以解决新烟碱杀虫剂抗性不断增加和对鳞翅目害虫的杀虫活性较低等问题。[方法]设计并化学合成一系列9个含有苄基的新型氮桥环新烟碱类化合物,并测试各个化合物的杀虫活性。[结果]总体而言,所合成化合物的杀虫活性均低于本课题组已报道过的苯胺系列氮桥环化合物。[结论]在新型氮桥环新烟碱类化合物的结构中引入柔性连接(CH_2)未能达到提高生物活性的目的。
[Aims ] The aim of this study is that, through introducing a flexible linker（CH_2） into the structure of azabridged neonicotinoids, we tried to find new neonicotinoid compounds to solve the problem of resistance and limited lepidopteran activities. [Methods ] A series of novel azabridged neonicotinoid analogues containing benzyl group were designed and synthesized, and their insecticidal activities were tested too. [Results ] The result is that insecticidal activities of nine compounds with new structurewere not as good as the phenylamine series of azabridged neonicotinoids reported by our group before. [Conclusions ] It can notincreasethe insecticidal activities byintroducing a flexible linkage（CH_2） into the structure of azabridged neonicotinoids.