Citation: Liu Yang, Liu Ming, Chen Minggui, Wu Changchun, Hua Xuewen, Zhou Sha, Wang Baolei, Li Zhengming. Design, Synthesis and Bioactivities of Novel Strobilurin Derivatives Containing 1, 3, 4-Oxadiazole Moity[J]. Chinese Journal of Organic Chemistry, ;2017, 37(2): 403-410. doi: 10.6023/cjoc201607029 shu

Design, Synthesis and Bioactivities of Novel Strobilurin Derivatives Containing 1, 3, 4-Oxadiazole Moity

  • Corresponding author: Li Zhengming, nkzml@vip.163.com
  • Received Date: 19 July 2016
    Revised Date: 12 September 2016

    Fund Project: the "111" Project of Ministry of Education of China B06005

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  • A series of novel strobilurin derivatives containing 1, 3, 4-oxdiazole moity were designed and synthesized based on the bioisosterism and coordination of active substructure theories. The structures of new compounds were characterized by 1H NMR, 13C NMR and HRMS spectra. The bioassay indicated that the fungicidal activities of some compounds against Sclerotinia sclerotiorum reached the activity of azoxystrobin as the control and some compounds against Rhizotonia cerealis in vitro were more effective than the same control. Their structure-activity relationship was discussed. Methyl (E)-2-(2-((4-(1, 3, 4-oxadiazol-2-yl) phenoxy) methyl) phenyl)-3-methoxyacrylate (Ⅱa) and methyl (E)-2-(2-((4-(5-ethyl-1, 3, 4-oxadiazol-2-yl) phe-noxy) methyl) phenyl)-3-methoxyacrylate (Ⅱc) could be considered as leading compounds for further investigation.
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