袁含笑, 张文广, 刘函如, 张云天, 张彩霞, 郭孜怡, 高艳清, 雷鹏, 刘西莉. 香豆素肟酯衍生物的合成及抑菌活性[J]. 农药学学报, 2022, 24(5): 1189-1195. DOI: 10.16801/j.issn.1008-7303.2022.0078
    引用本文: 袁含笑, 张文广, 刘函如, 张云天, 张彩霞, 郭孜怡, 高艳清, 雷鹏, 刘西莉. 香豆素肟酯衍生物的合成及抑菌活性[J]. 农药学学报, 2022, 24(5): 1189-1195. DOI: 10.16801/j.issn.1008-7303.2022.0078
    YUAN Hanxiao, ZHANG Wenguang, LIU Hanru, ZHANG Yuntian, ZHANG Caixia, GUO Ziyi, GAO Yanqing, LEI Peng, LIU Xili. Synthesis and antifungal activity of coumarin oxime esters[J]. Chinese Journal of Pesticide Science, 2022, 24(5): 1189-1195. DOI: 10.16801/j.issn.1008-7303.2022.0078
    Citation: YUAN Hanxiao, ZHANG Wenguang, LIU Hanru, ZHANG Yuntian, ZHANG Caixia, GUO Ziyi, GAO Yanqing, LEI Peng, LIU Xili. Synthesis and antifungal activity of coumarin oxime esters[J]. Chinese Journal of Pesticide Science, 2022, 24(5): 1189-1195. DOI: 10.16801/j.issn.1008-7303.2022.0078

    香豆素肟酯衍生物的合成及抑菌活性

    Synthesis and antifungal activity of coumarin oxime esters

    • 摘要: 为发现具有高抑菌活性的肟酯类化合物, 结合本课题组前期研究, 设计并合成了18个新型香豆素肟酯衍生物, 并对抑菌活性及构效关系进行了研究。离体生物活性测定结果表明, 目标化合物在50 μg/mL下对番茄灰霉病菌、苹果树腐烂病菌和水稻纹枯病菌均表现出一定的抑制活性, 其中化合物 4n 对番茄灰霉病菌和水稻纹枯病菌的EC50值分别为4.44 μg/mL和3.65 μg/mL,表现出比香豆素和肟菌酯更优或相似的活性。

       

      Abstract: In order to discover high antifungal activity oxime esters compound, based on our previous studies, 18 novel coumarin oxime esters were designed and synthesized. The antifungal activity was evaluated and the structure-activity relationship was analyzed. The in vitro bioassay results showed that the target compounds showed antifungal activities against Botrytis cinerea, Valsa mali and Rhizoctonia solani. Especially, compound 4n displayed excellent activity against B. cinerea (EC50 = 4.44 μg/mL) and R. solani (EC50 = 3.65 μg/mL), which are better than or similar to those of coumarin and trifloxystrobin.

       

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