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有机化学
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有机化学 ›› 2010, Vol. 30 ›› Issue (10): 1567-1573. 上一篇    下一篇

研究简报

一种结构新颖的苯并噻唑硫醚类化合物的合成及杀菌活性

赵培亮1,2，王福1，黄伟1，陈琼1，刘祖明*,1   

  1. (1华中师范大学化学学院 农药与化学生物学教育部重点实验室 武汉 430079)
    (2南方医科大学药学院 广州 510515)
  • 收稿日期:2009-07-24 修回日期:2010-01-26 发布日期:2010-05-25
  • 通讯作者: 刘祖明 E-mail:zmliu@mail.ccnu.edu.cn
  • 基金资助:

    国家级.国家自然科学基金

Synthesis and Fungicidal Activities of Novel Thioethers Containing Benzothiazole Moiety

Zhao Peiliang1,2 Wang Fu1 Huang Wei1 Chen Qiong Liu Zuming*,1   

  1. (1 Key Laboratory of Pesticide and Chemical Biology of Ministry of Education, College of Chemistry, Central China Normal University, Wuhan 430079)
    (2 School of Pharmaceutical Sciences, Southern Medical Universtiy, Guangzhou 510515)
  • Received:2009-07-24 Revised:2010-01-26 Published:2010-05-25
  • Contact: Zuming LIU E-mail:zmliu@mail.ccnu.edu.cn

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1242

被引次数

24 | 6

以各种取代苯并噻唑为侧链结构, 对Strobilurins 类杀菌剂苯噻菌酯的药效团部分进行修饰, 设计合成了18个结构新颖的苯并噻唑硫醚类化合物, 结构经1H NMR, MS, 元素分析确证. 并用X-ray 单晶衍射测定了化合物5,5-二甲基-4-甲氧基-3-[2-(苯并噻唑-2-硫甲基)苯基]-2(5H)-呋喃酮(6a)的晶体结构. 初步的生物活性测试结果表明, 在200 mg/L 的剂量下部分化合物表现出一定的杀菌活性.

关键词: 苯并噻唑, 合成, 杀菌活性, 晶体结构

Eighteen novel thioethers were designed and synthesized by modifying the pharmacophore of the strobilurin fungicide with various substituted benzothiazole rings as the side chain structure. Their structures were characterized by 1H NMR, MS techniques and elemental analysis, and the single crystal structure of compound 6a was determined by X-ray diffraction analysis. The preliminary bioassay showed that some of them exhibited certain fungicidal activities.

Key words: benzothiazole, synthesis, fungicidal activity, crystal structure