有机化学 ›› 2009, Vol. 29 ›› Issue (9): 1381-1386. 上一篇    下一篇

研究论文

新型含肟醚Strobilurins衍生物的合成及杀菌活性研究

柳爱平*,a,b 何海军a,b 刘兴平a 何 莲a 胡春华a,c
魏振中a,c 胡志彬a 黄明智a 欧晓明a 苏胜培b
  

  1. (a 湖南化工研究院 国家农药创制工程技术研究中心 长沙 410007)
    (b湖南师范大学 化学生物学及中药分析教育部重点实验室 长沙 410081)
    (c华中师范大学化学学院 武汉 430079)
  • 收稿日期:2008-12-24 修回日期:2009-02-26 发布日期:2009-12-30
  • 通讯作者: 柳爱平

Synthesis and Fungicidal Activities of Novel Oxime Ether Strobilurins

Liu, Aiping *,a,b He, Haijun a,b Liu, Xingping a He, Lian a Hu, Chunhua a,c
Wei, Zhenzhong a,c Hu, Zhibin a Huang, Mingzhi a Ou, Xiaoming a Su, Shengpei b
  

  1. (a National Engineering Research Center for Agrochemicals, Hunan Research Institute of Chemical Industry,
    Changsha 410007)
    (b Key Laboratory of Chemical Biology and Traditional Chinese Medicine Research, Ministry of Education,
    Hunan Normal University, Changsha 410081)
    (c College of Chemistry, Central China Normal University, Wuhan 430079)
  • Received:2008-12-24 Revised:2009-02-26 Published:2009-12-30
  • Contact: Liu, Aiping

Strobilurins类化合物具有优异的杀菌活性, 设计并合成了12个未见文献报道的含肟醚Strobilurins类衍生物, 其化学结构经1H NMR, IR, HPLC/MS和元素分析表征. 初步生物活性测定结果表明, 该类化合物具有良好的杀菌活性, 如6b~6d和6h在500 μg/mL浓度下对小麦白粉病菌的防效达90%以上, 同时, 6c和6d对稻瘟病菌的抑制率也达90%以上, 其中, 化合物6c在25 μg/mL的浓度下, 对小麦白粉病菌的防效仍达72%.

关键词: Strobilurins, 杀菌活性, 合成, 构效关系

Strobilurin derivatives have significant fungicidal activity, hence, twelve new strobilurin derivatives containing oxime ether moiety were designed and synthesized, and their structures were confirmed by 1H NMR, IR, HPLC/MS techniques and elemental analysis. Preliminary bioassay showed that most of these title compounds had potent fungicidal activity. For example, 6b~6d and 6h exhibited more than 90% ac-tivities against Blumeria graminis at a concentration of 500 μg/mL. Furthermore, compounds 6c and 6d also showed more than 90% inhibition against Pyricularia oryzae. Especially, compound 6c gave 72% control against Blumeria graminis at 25 μg/mL.

Key words: fungicidal activity, synthesis, structure-activity relationship, strobilurins