陈美航, 罗海荣, 杜士杰, 鲁道旺, 张迅, 沈祖敏, 秦旭峰, 谯登贤, 吴文能. 3-芳基-4-氧香豆素基苯基硫脲衍生物的合成及杀菌活性[J]. 农药学学报, 2021, 23(1): 76-82. DOI: 10.16801/j.issn.1008-7303.2021.0011
    引用本文: 陈美航, 罗海荣, 杜士杰, 鲁道旺, 张迅, 沈祖敏, 秦旭峰, 谯登贤, 吴文能. 3-芳基-4-氧香豆素基苯基硫脲衍生物的合成及杀菌活性[J]. 农药学学报, 2021, 23(1): 76-82. DOI: 10.16801/j.issn.1008-7303.2021.0011
    CHEN Meihang, LUO Hairong, DU Shijie, LU Daowang, ZHANG Xun, SHEN Zumin, QIN Xufeng, QIAO Dengxian, WU Wenenng. Synthesis and antibacterial activities of 3-aryl-4-coumarinoxy phenylthiourea derivatives[J]. Chinese Journal of Pesticide Science, 2021, 23(1): 76-82. DOI: 10.16801/j.issn.1008-7303.2021.0011
    Citation: CHEN Meihang, LUO Hairong, DU Shijie, LU Daowang, ZHANG Xun, SHEN Zumin, QIN Xufeng, QIAO Dengxian, WU Wenenng. Synthesis and antibacterial activities of 3-aryl-4-coumarinoxy phenylthiourea derivatives[J]. Chinese Journal of Pesticide Science, 2021, 23(1): 76-82. DOI: 10.16801/j.issn.1008-7303.2021.0011

    3-芳基-4-氧香豆素基苯基硫脲衍生物的合成及杀菌活性

    Synthesis and antibacterial activities of 3-aryl-4-coumarinoxy phenylthiourea derivatives

    • 摘要: 为寻找具有更高杀菌活性的含香豆素的硫脲类衍生物,本文合成了13个未见文献报道的3-芳基-4-氧香豆素基苯基硫脲衍生物,其结构经过红外光谱、核磁共振氢谱、核磁共振碳谱、质谱和元素分析确认,并初步测试了其对两种病原细菌的活性。结果表明:该类化合物具有较好的杀菌活性,其中化合物 4b4h4i4j4m 抑制水稻白叶枯菌Xanthomonas oryzae pv. oryzae的EC50值分别为117.7、118.1、105.7、104.3和110.5 μg/mL,优于对照药剂噻菌铜 (EC50值195.8 μg/mL);化合物 4b4h4i4j4m 抑制柑橘溃疡病菌Xanthomonas citri subsp. citri的EC50值分别为111.6、95.6、102.9、83.1和112.1 μg/mL,优于对照药剂噻菌铜 (EC50值128.7 μg/mL)。

       

      Abstract: In order to find thiourea derivatives containing coumarin moiety with high antibacterial activities, thirteen 3-aryl-4-coumarinoxy phenylthiourea derivatives were synthesized. Their structures were characterized by IR, 1H NMR, 13C NMR, MS and elemental analysis, and their antibacterial activities against two pathogenic bacteria were preliminarily evaluated in this work. The results indicated that target compounds possessed good antibacterial activities. Among of them, compounds 4b , 4h , 4i , 4j and 4m showed excellent antibacterial activities against Xanthomonas oryzae pv. oryzae with EC50 value of 117.7, 118.1, 105.7, 104.3 110.5 μg/mL, respectively, which were all superior to that of thiodiazole-copper (EC50 value 195.8 μg/mL). Meanwhile, compounds 4b , 4h , 4i , 4j and 4m showed better antibacterial activities against Xanthomonas citri subsp. citri with EC50 value of 111.6, 95.6, 102.9, 83.1, 112.1 μg/mL, respectively, which were superior to that of thiodiazole-copper (EC50 value 128.7 μg/mL).

       

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