Chinese Journal of Organic Chemistry >
Design, Synthesis and Activity Evaluation of Arylpyridone Hydrazones
Received date: 2018-10-16
Revised date: 2018-12-05
Online published: 2018-12-28
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.
Wang Jiayao , Tao Han , Jin Mi , Li Lisha , Xiao Yumei , Li Jiaqi , Qin Zhaohai . Design, Synthesis and Activity Evaluation of Arylpyridone Hydrazones[J]. Chinese Journal of Organic Chemistry, 2019 , 39(4) : 1044 -1052 . DOI: 10.6023/cjoc201810019
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