高等学校化学学报 ›› 2014, Vol. 35 ›› Issue (8): 1703.doi: 10.7503/cjcu20131258

• 有机化学 • 上一篇    下一篇

芳亚甲基硝基缩氨基胍类化合物的合成及杀虫活性

杨冬燕1, 王蕾1, 贾长青1, 李长胜3, 马永强1(), 芮昌辉2, 徐彦军1, 覃兆海1   

  1. 1. 中国农业大学理学院, 北京 100193
    2. 中国农业科学院植物保护研究所, 北京 100193
    3. 佳木斯大学药学院, 佳木斯 154007
  • 收稿日期:2013-12-23 出版日期:2014-08-10 发布日期:2019-08-01
  • 作者简介:联系人简介: 马永强, 男, 博士, 教授, 博士生导师, 主要从事新农药创制研究. E-mail: myqliang@iccas.ac.cn
  • 基金资助:
    国家自然科学基金(批准号: 31272076)和农业部行业专项项目(批准号: 201203022)资助

Syntheses and Insecticidal Activities of Nitro Arylideneamino Guanidine Derivatives

YANG Dongyan1, WANG Lei1, JIA Changqing1, LI Changsheng3, MA Yongqiang1,*(), RUI Changhui2, XU Yanjun1, QIN Zhaohai1,*   

  1. 1. College of Science, China Agricultural University, Beijing 100193, China
    2. Institute of Plant Prorection, China Academy of Agriculture Science, Beijing 100193, China
    3. College of Pharmacy, Jiamusi University, Jiamusi 154007, China
  • Received:2013-12-23 Online:2014-08-10 Published:2019-08-01
  • Contact: MA Yongqiang,QIN Zhaohai E-mail:myqliang@iccas.ac.cn
  • Supported by:
    Supported by the National Natural Science Foundation of China(No.31272076) and the Project of the Ministry of Agriculture and Special Industries of China(No.201203022)

摘要:

依据活性亚结构拼接原理, 以硝基胍为原料, 合成了一系列具有新烟碱类和缩氨基脲类杀虫剂共同结构特征的芳亚甲基硝基缩氨基胍类化合物, 其结构通过1H NMR、 IR和元素分析等方法进行了确证. 杀虫活性测定结果表明, 在600 μg/mL浓度下, 目标化合物对桃蚜[Myzuspersicae(Sulzer)]具有较优异的活性, 其中化合物4-2, 4-8, 4-10, 4-16, 4-27, 4-31和4-34的校正死亡率均在90%以上. 进一步以桃蚜、 棉蚜(Aphis gossypii)和桃粉蚜(Hyalopterusamygdali blanchard)为对象, 测定了化合物4-2, 4-8和4-34的精密毒力. 结果表明, 它们在低浓度下仍然具有很高的活性, 其中化合物4-8对棉蚜的活性甚至优于对照药剂吡虫啉, 在3.13 μg/mL浓度下致死率仍高达95.7%(吡虫啉为79.4%), 具有进一步研究开发的价值.

关键词: 芳亚甲基硝基缩氨基胍, 蚜虫, 杀虫活性

Abstract:

In order to search for better lead compounds with excellent biological activities, a novel series of acyclic neonicotinoids of nitro arylideneamino guanidine derivatives was designed and synthesized from nitroaminoguanidine by the method of linking the active substructures of neonicotiniod insecticides and semicarbazone insecticides. All the target compounds were confirmed by 1H NMR, IR and elemental analysis. The preliminary bioassay showed that the lethal rates of target compounds to Myzuspersicae were excellent at the concentration of 600 μg/mL. The lethal rates of several compounds, such as 4-2, 4-8, 4-10, 4-16, 4-27, 4-31 and 4-34, were more than 90%. Further research of compounds 4-2, 4-8 and 4-34 against Myzuspersicae, Aphis gossypii and Hyalopterusamygdali blanchard indicated these compounds possessed high activity at low concentrations, especially, the activity of compound 4-8 was better than that of imidacloprid against Hyalopteraamygdali blanchard, its lethal rate was 95.7% compared to imidacloprid(79.4%) at the concentration of 3.13 μg/mL, which confirmed that this compound is worth of research.

Key words: Arylideneamino guanidine derivative, Aphid, Insecticidal activity

中图分类号: 

TrendMD: