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2020 , Vol. 40 >Issue 6: 1772 - 1778

DOI: https://doi.org/10.6023/cjoc202001028

研究简报

新型含噁唑单元的吡唑酰胺衍生物的合成及其生物活性

  • 张敏 ,
  • 郑丹丹 ,
  • 倪亚丹 ,
  • 梁凯 ,
  • 荀校 ,
  • 胡兰萍 ,
  • 陈庆文 ,
  • 杨冰 ,
  • 梁志鹏 ,
  • 丁颖 ,
  • 石健 ,
  • 戴红
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  • a 南通大学化学化工学院 江苏南通 226019;
    b 南通大学分析测试中心 江苏南通 226019

收稿日期: 2020-01-20

  修回日期: 2020-02-27

  网络出版日期: 2020-03-06

基金资助

国家自然科学基金（No.21372135）、南通市科技计划（No.MS12019060）资助项目.

收起

Synthesis and Bioactivities of Novel Pyrazole Amides Carrying Oxazole Moiety

  • Zhang Min ,
  • Zheng Dandan ,
  • Ni Yadan ,
  • Liang Kai ,
  • Xun Xiao ,
  • Hu Lanping ,
  • Chen Qingwen ,
  • Yang Bing ,
  • Liang Zhipeng ,
  • Ding Ying ,
  • Shi Jian ,
  • Dai Hong
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  • a College of Chemistry and Chemical Engineering, Nantong University, Nantong, Jiangshu 226019;
    b Analysis and Testing Center, Nantong University, Nantong, Jiangshu 226019

Received date: 2020-01-20

  Revised date: 2020-02-27

  Online published: 2020-03-06

Supported by

Project supported by the National Natural Science Foundation of China (No. 21372135) and the Science and Technology Project Fund of Nantong City (No. MS12019060).

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摘要

为了寻找具有良好生物活性的吡唑酰胺化合物，基于氯虫苯甲酰胺的结构，在吡唑环的5-位引入取代噁唑环单元，合成出了一系列新型吡唑酰胺，利用1H NMR，13C NMR和元素分析对其目标产物的结构进行了确证.生测结果表明，所有目标化合物在500 μg/mL时对粘虫均显示出较好的杀虫活性（致死率≥ 90%）.5个化合物在100 μg/mL时对粘虫的防治效果可达90%~100%，3个化合物在100 μg/mL时对苜蓿蚜的杀死率为90%~100%.另外，2个化合物在500 μg/mL时对朱砂叶螨的防效可达80%~100%.

关键词： 噁唑; 吡唑酰胺; 合成; 生物活性

本文引用格式

张敏 , 郑丹丹 , 倪亚丹 , 梁凯 , 荀校 , 胡兰萍 , 陈庆文 , 杨冰 , 梁志鹏 , 丁颖 , 石健 , 戴红 . 新型含噁唑单元的吡唑酰胺衍生物的合成及其生物活性[J]. 有机化学, 2020 , 40(6) : 1772 -1778 . DOI: 10.6023/cjoc202001028

Abstract

In order to find new pyrazole amides with wonderful bioactivities, a series of novel pyrazole amide derivatives were synthesized by introducing substituted oxazole ring into the C-5 position of pyrazole skeleton based on the lead chlorantraniliprole. The aimed compounds were structurally characterized through 1H NMR, 13C NMR and elemental analysis. The preliminary bioassay results exhibited that all the title compounds displayed more than 90% insecticidal activities against Mythimna separata (Walker) at 500 μg/mL. At the dosage of 100 μg/mL, five compounds possessed 90%~100% insecticidal activities against Mythimna separata (Walker), and three compounds exhibited insecticidal property against Aphis craccivora with 90%~100%. Additionally, at the dosage of 500 μg/mL, two compounds possessed insecticidal activity against Tetranychus cinnabarinus with 80%~100%.

Key words： oxazole; pyrazole amide; synthesis; bioactivity

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