有机化学 ›› 2016, Vol. 36 ›› Issue (1): 158-164.DOI: 10.6023/cjoc201507009 上一篇    下一篇

研究论文

含氮杂吲哚骨架的噻唑啉化合物的合成和抗菌活性

麻红利a, 闫晓静b, 肖玉梅a, 袁德凯a, 张振华a, 傅滨a, 袁会珠b   

  1. a 中国农业大学应用化学系 北京 100193;
    b 中国农业科学院植物保护研究所 北京 100193
  • 收稿日期:2015-07-12 修回日期:2015-08-19 出版日期:2016-01-25 发布日期:2015-09-17
  • 通讯作者: 傅滨 E-mail:fubinchem@cau.edu.cn
  • 基金资助:

    国家“十二五”科技支撑计划(No. 2011BAE06B02)、国家自然科学基金(No. 21172255)资助项目.

Synthesis and Fungicidal Activities of Azaindolyl Thiazoline Compounds

Ma Honglia, Yan Xiaojingb, Xiao Yumeia, Yuan Dekaia, Zhang Zhenhuaa, Fu Bina, Yuan Huizhub   

  1. a Department of Applied Chemistry, China Agricultural University, Beijing 100193;
    b Institute of Plant Protection, Chinese Academy of Agricultural Science, Beijing 100193
  • Received:2015-07-12 Revised:2015-08-19 Online:2016-01-25 Published:2015-09-17
  • Supported by:

    Project supported by the National S&T Pillar Program of China (No. 2011BAE06B02), and the National Natural Science Foundation of China (No. 21172255).

为寻找新的高活性的农用杀菌剂, 通过活性拼接原理, 设计合成了20个未见文献报道的氮杂吲哚噻唑啉化合物, 并通过光谱方法确证结构, 在50 mg/L浓度下, 部分标题化合物显示出比较好的植物杀菌活性. 进一步的活性测试表明 2a2d对芦笋茎枯和稻瘟病菌的EC50值达到6.55和9.66 mg/L, 优于或相当于对照药剂, 能够作为创制新型杀菌剂的先导化合物.

关键词: 氮杂吲哚, 噻唑(啉), 合成, 抗菌活性

In order to find new agrochemical products with high activities, 20 azaindolyl thiazoline compounds were designed and synthesized, and their structures were identified by spectral methods. At the concentration of 50 mg/L, some of the title compounds showed good fungicidal activities. Among those compounds, the EC50 values of 2a and 2d against Phomopsis asparagi and Pyricularia oryzae Cav are 6.55 and 9.66 mg/L, which are superior or comparable to the control pesticides, then they can serve as the lead compounds for new fungicide discovery.

Key words: azaindolyl, thiazoline, synthesis, fungicidal activity