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2018 , Vol. 38 >Issue 9: 2450 - 2457

DOI: https://doi.org/10.6023/cjoc201806030

研究简报

新型含取代吡啶结构的吡唑酰胺类化合物的合成与生物活性研究

  • 石玉军 ,
  • 周钱 ,
  • 王杨 ,
  • 钱宏炜 ,
  • 叶林玉 ,
  • 冯霞 ,
  • 陈辉 ,
  • 李雅婷 ,
  • 戴红 ,
  • 魏中昊 ,
  • 吴锦明
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  • a 南通大学化学化工学院 南通 226019;
    b 南通大学杏林学院 南通 226008

收稿日期: 2018-06-20

  修回日期: 2018-07-19

  网络出版日期: 2018-08-14

基金资助

国家自然科学基金（No.21372135）、江苏省"六大人才高峰"（No.2013-SWYY-013）、南通市科技计划（No.MS22015020）、江苏省大学生创新训练计划（No.201810304016Z）和南通大学杏林学院科研基金（No.2016K130）资助项目.

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Synthesis and Biological Activities of Novel Pyrazole Amide Derivatives Containing Substituted Pyridyl Group

  • Shi Yujun ,
  • Zhou Qian ,
  • Wang Yang ,
  • Qian Hongwei ,
  • Ye Linyu ,
  • Feng Xia ,
  • Chen Hui ,
  • Li Yating ,
  • Dai Hong ,
  • Wei Zhonghao ,
  • Wu Jinming
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  • a College of Chemistry and Chemical Engineering, Nantong University, Nantong 226019;
    b Xinglin College, Nantong University, Nantong 226008

Received date: 2018-06-20

  Revised date: 2018-07-19

  Online published: 2018-08-14

Supported by

Project supported by the National Natural Science Foundation of China (No. 21372135), the Research Foundation of the Six People Peak of Jiangsu Province (No. 2013-SWYY-013), the Science and Technology Project Fund of Nantong City (No. MS22015020), the Science and Technology Innovation Foundation for the College Students of Jiangsu Province (No. 201810304016Z) and the Science Foudation of Nantong University Xinglin College (No. 2016K130).

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摘要

为了从吡唑酰胺类化合物中寻找新的活性物质，采用活性基团拼接原理，设计并合成了一系列未见文献报道的新型含取代吡啶结构的吡唑酰胺类衍生物.初步的生物活性测定结果显示，部分目标化合物表现出较好的杀虫活性.在测试浓度为500 μg/mL时，10个化合物对粘虫的杀死率可达60%~100%，1个化合物对蚜虫的杀死率为100%.当测试浓度降至100 μg/mL时，2个化合物对粘虫的杀死率可达70%~100%，高于对照药唑虫酰胺的防效.此外，当测试浓度降至20 μg/mL时，1个化合物对粘虫的杀死率为50%.

关键词： 吡啶; 吡唑酰胺; 合成; 生物活性

本文引用格式

石玉军 , 周钱 , 王杨 , 钱宏炜 , 叶林玉 , 冯霞 , 陈辉 , 李雅婷 , 戴红 , 魏中昊 , 吴锦明 . 新型含取代吡啶结构的吡唑酰胺类化合物的合成与生物活性研究[J]. 有机化学, 2018 , 38(9) : 2450 -2457 . DOI: 10.6023/cjoc201806030

Abstract

In order to find novel pyrazole amides having potent bioactivities, a series of novel pyrazole amide compounds carrying substituted pyridyl moiety were designed and synthesized according to the method of active substructure combination. The preliminary bioassay data showed that some title compounds displayed good insecticidal activities. At the concentration of 500 μg/mL, ten compounds exhibited insecticidal activity against Oriental armyworm with 60%~100%, and one compound indicated insecticidal activity against Aphis medicaginis with 100%. When the concentration was reduced to 100 μg/mL, two compounds still showed insecticidal activity against Oriental armyworm with 70%~100%, which were better than that of the control tolfenpyrad. Additionally, one compound displayed 50% insecticidal activity against Oriental armyworm at the concentration of 20 μg/mL.

Key words： pyridine; pyrazole amide; synthesis; bioactivity

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