节点文献

Aspernigerin类似物的合成及生物活性研究

Synthesis and Bioactivity of Aspernigerin Analogues

  • 推荐 CAJ下载
  • PDF下载
  • 不支持迅雷等下载工具,请取消加速工具后下载。

【作者】 吴清来李永强杨新玲凌云

【Author】 Wu,Qinglaia Li,Yongqiangb Yang,Xinlinga Ling,Yun,a(aKey Laboratory of Pesticide Chemistry and Application,Ministry of Agriculture,Department of Applied Chemistry,College of Science,China Agricultural University,Beijing 100193)(bState Key Laboratory of Elemento-Organic Chemistry,Nankai University,Tianjin 300071)

【机构】 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南开大学元素有机化学国家重点实验室

【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.

【Abstract】 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.

【基金】 国家自然科学基金(No.21072222);国家973计划(No.2010CB126104)资助项目~~
  • 【文献出处】 有机化学 ,Chinese Journal of Organic Chemistry , 编辑部邮箱 ,2012年04期
  • 【分类号】TQ450.1
  • 【被引频次】11
  • 【下载频次】211
节点文献中: 

本文链接的文献网络图示:

本文的引文网络