有机化学 ›› 2018, Vol. 38 ›› Issue (12): 3363-3372.DOI: 10.6023/cjoc201807001 上一篇    下一篇

研究简报

多杀菌素A衍生物的合成及其生物活性研究

张凯a, 李加荣a, 温都苏a, 刘洪林b, 王海邮b, 阿拉木斯b   

  1. a 北京理工大学化学与化工学院 北京 100081;
    b 中国农业科学院草原研究所 呼和浩特 010000
  • 收稿日期:2018-07-01 修回日期:2018-08-02 发布日期:2018-09-05
  • 通讯作者: 李加荣 E-mail:jrli@bit.edu.cn
  • 基金资助:

    国家自然科学基金(No.41471198)资助项目.

Study on the Synthesis and Insecticidal Activity of Spinosyn A Derivatives

Zhang Kaia, Li Jiaronga, Wen Dusua, Liu Honglinb, Wang Haiyoub, A Lamusib   

  1. a School of Chemistry and Chemical Engineering, Beijing Institute of Technology, Beijing 100081;
    b Institute of Grassland Research of Chinese Academy of Agricultural Sciences, Hohhot 010000
  • Received:2018-07-01 Revised:2018-08-02 Published:2018-09-05
  • Contact: 10.6023/cjoc201807001 E-mail:jrli@bit.edu.cn
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 41471198).

多杀菌素(Spinosyns)是一类由放线菌刺糖多孢菌发酵产生的新型生物杀虫剂,因其具有广谱高效、对环境和非靶标动物毒性小等优点,已经被广泛应用于农业的虫害防治中.为了寻找更高效的杀虫剂,合成了一系列多杀菌素A C-17位不同取代基的衍生物,并测定了对小菜蛾的杀虫活性.所合成的衍生物均对小菜蛾表现出不错的杀虫活性.

关键词: 天然产物, 多杀菌素A, 半合成衍生物, 杀虫活性

Spinosyns are a novel kind of biopesticide produced by Saccharopolyspora spinosa. Spinosyns have been widely applied in pest control because of their broad insecticidal spectrum, high insecticidal activity, low environmental impact, and low toxicity. To identify spinosyn compounds with improved insecticidal activity, a series of D-forosamine replacement derivatives of spinosyn A were synthesized. The insecticidal activities of the synthetic derivatives were evaluated against 3rd-instar larvae of Plutella xylostella. All derivatives exhibited good insecticidal activity to P. xylostella.

Key words: natural product, spinosyn A, semi-synthetic derivative, insecticidal activity