In order to develop thiourea derivatives with antibacterial activities, a series of novel 1-aryl-3-(3-((2-oxo-2H-chromen-4-yl)oxy)phenyl)thiourea derivative was synthesized from 4-hydroxycoumarin via chlorination, etherification, isothiocyanate formation and addition reactions.The structures of the title compounds were characterized by infrared spectroscopy(IR), nuclear magnetic resonance spectrocopy(NMR) and mass spectrometry(MS).The results show that title compounds exhibit excellent antibacterial activities against Xanthomonas oryzae pv.oryzae(Xoo) and Xanthomonas citri subsp.Citri(Xcc).Among of them, compounds 4k, 4l, 4m and 4n show excellent antibacterial activities against Xoo, with the EC50 values 137.42, 131.05, 129.23 and 117.43 mg/L, respectively, which were better than that of the control agent thiodiazole-copper(195.24 mg/L).Compounds 4k, 4l, 4m and 4n display considerable antibacterial activities against Xcc, with the EC50 values of 97.02, 94.31, 102.28 and 90.52 mg/L, respectively, which are better than that of thiodiazole-copper(120.25 mg/L).%为了筛选出具有较高抑菌活性的含香豆素的硫脲类衍生物,本文以4-羟基香豆素为原料,经氯化、醚化、异硫氰酸化和加成反应合成了一系列1-芳基-3-(3-(4-氧香豆素基)苯基)硫脲衍生物,其结构经红外光谱(IR)、核磁共振谱(NMR)和质谱(MS)等技术手段进行了表征. 结果表明,目标化合物对水稻白叶枯菌和柑橘溃疡菌均具有较好的抑制活性. 其中化合物4k、4l、4m和4n抑制水稻白叶枯菌活性EC50值分别为137.42、131.05、129.23和117.43 mg/L,优于对照药剂噻菌铜的活性 (195.24 mg/L);化合物4k、4l、4m和4n抑制柑橘溃疡菌活性EC50值分别为97.02、94.31、102.28和90.52 mg/L,优于噻菌铜的活性(120.25 mg/L).
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