Chin. J. Org. Chem. ›› 2019, Vol. 39 ›› Issue (4): 1044-1052.DOI: 10.6023/cjoc201810019 Previous Articles     Next Articles

Articles

芳基吡啶酮腙类化合物的设计、合成及杀菌活性研究

王家尧, 陶晗, 金蜜, 李丽莎, 肖玉梅, 李佳奇, 覃兆海   

  1. 中国农业大学理学院 北京 100193
  • 收稿日期:2018-10-16 修回日期:2018-12-05 出版日期:2019-04-25 发布日期:2018-12-28
  • 通讯作者: 覃兆海 E-mail:qinzhaohai@263.net
  • 基金资助:

    国家自然科学基金(No.21572265)资助项目.

Design, Synthesis and Activity Evaluation of Arylpyridone Hydrazones

Wang Jiayao, Tao Han, Jin Mi, Li Lisha, Xiao Yumei, Li Jiaqi, Qin Zhaohai   

  1. College of Science, China Agricultural University, Beijing 100193
  • Received:2018-10-16 Revised:2018-12-05 Online:2019-04-25 Published:2018-12-28
  • Contact: 10.6023/cjoc201810019 E-mail:qinzhaohai@263.net
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No.21572265).

A series of novel arylpyridone hydrazones were designed and synthesized by using arylpyridinylmethanone as the plug-in molecules and ferimzone as parent compound. The structure of the products were confirmed by 1H NMR, 13C NMR and HRMS. The antifungal activities of all compounds were tested by growth rate method in vitro. The results showed that most of the compounds inhibited eight selected pathogens at the concentration of 70 μmol/L. The inhibitory effect of 2'-methylacetylbenzene-4,6-dimethoxypyrimidine-2-hydrazone (Ⅲ-3) and 2-(2'-((4'-bromo-phenyl)(3'-chloro-pyridine-4'-yl)-methylene-hydrazine)-4,6-dimethoxypyrimidine (Ⅲ-18) on pathogenic fungi was significantly higher than that of ferimzone, in which compound Ⅲ-3 has a great degree of inhibition on Botrytis cinerea with EC50 value of 22.18 μmol/L, and EC50 value of compound Ⅲ-18 is less than 0.35 umol/L on Thanatephorus cucumeris, which is 260 times higher than that of control.

Key words: plug-in molecule, arylpyridinylmethanone, arylpyridone hydrazone, antifungal activity