Study of Synthesis and Biological Activities of a Novel Macrolide Derivatives

doi:10.6023/cjoc201405007

Chin. J. Org. Chem. ›› 2014, Vol. 34 ›› Issue (12): 2543-2550.DOI: 10.6023/cjoc201405007 Previous Articles Next Articles

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一类新型大环内酯衍生物的合成及其生物活性研究

史大昕^a, 冯雪^a, 庄晓磊^a, 柴洪新^a, 刘霆^b, 张奇^a, 李加荣^a

a. 北京理工大学化工与环境学院北京 100081;
b. 北京市农林科学研究院北京 100097

收稿日期:2014-05-06 修回日期:2014-07-28 发布日期:2014-08-11
通讯作者: 张奇, 李加荣 E-mail:zhangqi@bit.edu.cn;jrli@bit.edu.cn
基金资助:
北京理工大学基础研究基金(No.20131042006)资助项目.

Study of Synthesis and Biological Activities of a Novel Macrolide Derivatives

Shi Daxin^a, Feng Xue^a, Zhuang Xiaolei^a, Chai Hongxin^a, Liu Ting^b, Zhang Qi^a, Li Jiarong^a

a. School of Chemical Engineering and Environment, Beijing institute of Technology, Beijing 100081;
b. Beijing Academy of Agricultural and Forestry Sciences, Beijing 100097

Received:2014-05-06 Revised:2014-07-28 Published:2014-08-11
Supported by:
Project supported by the Basic Research Fund of Beijing Institute of Technology (No. 20131042006).

Modification of molecular structure of pesticides is a common method to seek new efficient broad-spectrum insecticides. This study focused on modifying the structure of deglycosylated or partially deglycosylated spinosad. Eight new macrolide derivatives had been synthesized by acylation. Their structures were characterized by ¹H NMR, ¹³C NMR and MS techniques. Their fungicidal and insecticidal activities were also evaluated. The results showed that all compounds synthesized had excellent insecticidal activities against lepidoptera, coleoptera, diptera, hemiptera and nematoda. Compound 3e at the concentration of 100 mg/L presented 100% insecticidal activity against hemiptera (e.g. Myzus persicae) and compounds 3f and 3h loading 200 μg presented certain inhibition against pseudomonas.

Key words: macrolide, acylate, insecticidal activity, fungicidal activity

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Shi Daxin, Feng Xue, Zhuang Xiaolei, Chai Hongxin, Liu Ting, Zhang Qi, Li Jiarong. Study of Synthesis and Biological Activities of a Novel Macrolide Derivatives[J]. Chin. J. Org. Chem., 2014, 34(12): 2543-2550.

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一类新型大环内酯衍生物的合成及其生物活性研究

Study of Synthesis and Biological Activities of a Novel Macrolide Derivatives

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