Aspernigerin类似物的合成及生物活性研究  

Synthesis and Bioactivity of Aspernigerin Analogues

作　　者：吴清来[1] 李永强[2] 杨新玲[1] 凌云[1] 

机构地区：[1]中国农业大学理学院应用化学系农业部农药化学与应用重点开放实验室,北京100193 [2]南开大学元素有机化学国家重点实验室,天津300071

出　　处：《有机化学》2012年第4期747-754,共8页Chinese Journal of Organic Chemistry

基　　金：国家自然科学基金(No.21072222);国家973计划(No.2010CB126104)资助项目~~

摘　　要：以天然产物Aspernigerin为先导,将Aspernigerin结构中的一个1,2,3,4-四氢喹啉基团以芳胺类化合物替代,设计合成了15个未见文献报道的Aspernigerin类似物,结构均经过1H NMR,IR和元素分析确证.初步生物活性测试表明,大部分目标化合物均表现出了一定的杀虫和杀菌活性,其中化合物2n在200μg/mL的浓度下对小菜蛾仍表现出100%的杀虫活性,优于先导Aspernigerin和对照药剂噻虫嗪;化合物2d,2e,2j,2k表现出对黄瓜灰霉病优于先导Aspernigerin的抑制活性.Using natural product aspernigerin as the lead compound,fifteen new compounds were designed and synthesized by replaced one 1,2,3,4-tetrahydroquinoline group of aspernigerin with aromatic amine.Those structures were confirmed by 1H NMR,IR spectra and elemental analysis.The preliminary bioassay showed that most of the compounds exhibited certain fungicidal activities and insecticidal activities.In particular,compound 2n showed the most potent bioactivity against Plutella xylostella with the rate of 100% at the concentration of 200 μg/mL,better than aspernigerin and commercial insecticide thiamethoxam,and compounds 2d,2e,2j,2k showed higher inhibition effects against Botrytis cinerea than aspernigerin.

关 键 词：Aspernigerin 类似物 合成 1 2 3 4-四氢喹啉 芳胺 生物活性 

分 类 号：TQ450.1[化学工程—农药化工]