高等学校化学学报

高等学校化学学报 ›› 2004, Vol. 25 ›› Issue (9): 1657.

• 研究论文 • 上一篇    下一篇

[反]-β-法尼烯类似物的设计、合成与生物活性研究

杨新玲1, 黄文耀1, 凌云1, 阚伟2, 方宇凌2, 张钟宁2   

  1. 1. 中国农业大学应用化学系, 北京100094;
    2. 中国科学院动物研究所, 北京100080
  • 收稿日期:2003-07-21 出版日期:2004-09-24 发布日期:2004-09-24
  • 基金资助:

    国家“九五”科技攻关项目(批准号:97-563-02-06);农业部农药化学及应用技术重点开放实验室开放课题资助

Design, Synthesis and Biological Activity of EBF Analogues

YANG Xin-Ling1, HUANG Wen-Yao1, LING Yun1, KAN Wei2, FANG Yu-Ling2, ZHANG Zhong-Ning2   

  1. 1. Department of Applied Chemistry, China Agricultural University, Bejing 100094, China;
    2. Institute of Zoology, Chinese Academy of Sciences, Beijing 100080, China
  • Received:2003-07-21 Online:2004-09-24 Published:2004-09-24

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摘要： 对[反]-β-法尼烯(EBF)类似物的骨架结构原子进行改造,引入吡虫啉系列活性基团,设计合成了13个结构新颖的EBF类似物,并对其生物活性进行了研究.结果表明,这些化合物对蚜虫具有明显的抑制活性,尤其在低浓度时活性更明显,如质量浓度为25mg/L时,I10和I13对蚜虫的抑制率分别为93.1%和87.1%,远高于同浓度下吡虫啉的抑制率(66.7%).

关键词: [反]-&beta, -法尼烯, [反]-&beta, -法尼烯类似物, 合成, 生物活性

Abstract: Based on the features of active structures of (E)-β-farnesene(EBF) analogues summarized by Nishino and Bowers, 13 compounds(Ⅰ1-Ⅰ13) with a novel framework were designed by the method of linking active sub-structures which had the active framework of EBF analogues and the active structure of Neonicotinoid insecticide analogues. Thus, the target compounds were prepared in 24%-59% yield through 2-3 step reactions from the starting material geraniol. Their structures were confirmed by IR, 1H NMR, and MS. The results of bioassay demonstrated that most of the compounds show an obvious activity against adult Lipaphis erysimi at the test concentration. Especially at a lower concentration, some of them had a better activity than imidacloprid. For example, Ⅰ10 and Ⅰ13 exhibited respectively 93.1% and 87.1%, but imidacloprid showed 66.7% inhibiting rate at 25 mg/L.

Key words: EBF, EBF analogues, Synthesis, Biological activity

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