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有机化学
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有机化学 ›› 2010, Vol. 30 ›› Issue (05): 719-725. 上一篇    下一篇

研究论文

N-(取代噻唑-2-基)-菊酰胺类化合物的合成及生物活性研究

赵金浩，周勇，徐旭辉，朱烈，朱国念，程敬丽   

  1. (浙江大学农业与生物技术学院农药与环境毒理研究所 杭州 310029)
  • 收稿日期:2009-05-12 修回日期:2009-09-28 发布日期:2009-12-24
  • 通讯作者: 程敬丽 E-mail:chengjingli@zju.edu.cn

Synthesis and Biological Activities of N-(Substituted- thiazole-2-yl)-chrysanthemumamide

ZHAO Jin-Hao, ZHOU Yong, XU Xu-Hui, ZHU Lie, ZHU Guo-Nian, CHENG Jing-Li   

  1. (College of Agriculture and Biotechnology, Zhejiang University, Hangzhou 310029)
  • Received:2009-05-12 Revised:2009-09-28 Published:2009-12-24
  • Contact: Cheng Jing-Li E-mail:chengjingli@zju.edu.cn

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被引次数

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为了寻求新颖的氨基噻唑类先导化合物, 以含各种取代基的2-氨基噻唑在其氨基位置与拟除虫菊酯类农药的活性基团--菊酸采用亚结构对接的方法合成了35个N-(取代噻唑-2-基)-菊酰胺类化合物, 经1H NMR, ESI-MS和元素分析对化合物的结构进行了表征. 初步生物活性测定表明, 化合物3d, 6a, 6d, 4a, 4b, 4c, 4e在600 mg/L下对小菜蛾具有100%的杀虫活性, 化合物3d和7c在50 mg/L下对多种常见病原菌具有显著的杀菌活性, 全部化合物没有明显的除草活性.

关键词: N-取代噻唑菊酰胺, 杀虫活性, 杀菌活性

In order to find new thiazole lead compounds, thirty five N-(substituted-thiazole-2-yl)-chrysanthemumamides were synthesized from five types of chrysanthemic acids with seven substituted 2-amino-thiazols. The structures of all new compounds were confirmed by 1H NMR, MS and elemental analysis. At the concentration of 600 mg/L, compound 3d, 6a, 6d, 4a, 4b, 4c, 4e showed insecticidal activity (100%) against Plutella xylostella Linnaeus. At the concentration of 50 mg/L, compound 3d and 7c possessed good fungicidal activity toward the tested pathogens. All compounds have shown no herbicidal activity.

Key words: N-(substituted-thiazole-2-yl)-chrysanthemumamide, insecticidal activity, fungicidal activity