Bulletin of the Korean Chemical Society

Korean Chemical Society (대한화학회)
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Design, Synthesis and Antifungal Activities of Novel Strobilurin Derivatives Containing Pyrimidine Moieties

  • Zhang, Xiang (Research Center for Eco-Environmental Sciences, Chinese Academy of Sciences) ;
  • Gao, Yong-Xin (Research Center for Eco-Environmental Sciences, Chinese Academy of Sciences) ;
  • Liu, Hui-Jun (Research Center for Eco-Environmental Sciences, Chinese Academy of Sciences) ;
  • Guo, Bao-Yuan (Research Center for Eco-Environmental Sciences, Chinese Academy of Sciences) ;
  • Wang, Hui-Li (Research Center for Eco-Environmental Sciences, Chinese Academy of Sciences)
  • Received : 2012.03.13
  • Accepted : 2012.05.14
  • Published : 2012.08.20
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Abstract

Strobilurins are one of the most important classes of agricultural fungicides. To discover new strobilurin derivatives with high activity against resistant pathogens, a series of novel ${\beta}$-methoxyacrylate analogues were designed and synthesized by integrating substituted pyrimidine with a strobilurin pharmacophore. The compounds were confirmed and characterized by infrared, $^1H$ nuclear magnetic resonance, elemental analysis and mass spectroscopy. The bioassays indicated that most of the compounds (1a-1h) exhibited potent antifungal activities against Colletotrichum orbiculare, Botrytis cinerea Pers and Phytophthora capsici Leonian at the concentration of 50 ${\mu}g/mL$. Exhilaratingly, compound 1d (R=3-trifluoromethylphenyl) showed better antifungal activity against all the tested fungi than the commercial strobilurin fungicide azoxystrobin.

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