杜琳, 张斌, 宁磊, 王思敏, 路慧哲, 张建军, 董燕红. 含三唑结构的环己甲酰胺衍生物的合成及杀菌活性[J]. 农药学学报, 2020, 22(4): 595-601. DOI: 10.16801/j.issn.1008-7303.2020.0081
    引用本文: 杜琳, 张斌, 宁磊, 王思敏, 路慧哲, 张建军, 董燕红. 含三唑结构的环己甲酰胺衍生物的合成及杀菌活性[J]. 农药学学报, 2020, 22(4): 595-601. DOI: 10.16801/j.issn.1008-7303.2020.0081
    DU Lin, ZHANG Bin, NING Lei, WANG Simin, LU Huizhe, ZHANG Jianjun, DONG Yanhong. Synthesis and fungicidal activity of cyclohexanamide derivatives with triazole moeity[J]. Chinese Journal of Pesticide Science, 2020, 22(4): 595-601. DOI: 10.16801/j.issn.1008-7303.2020.0081
    Citation: DU Lin, ZHANG Bin, NING Lei, WANG Simin, LU Huizhe, ZHANG Jianjun, DONG Yanhong. Synthesis and fungicidal activity of cyclohexanamide derivatives with triazole moeity[J]. Chinese Journal of Pesticide Science, 2020, 22(4): 595-601. DOI: 10.16801/j.issn.1008-7303.2020.0081

    含三唑结构的环己甲酰胺衍生物的合成及杀菌活性

    Synthesis and fungicidal activity of cyclohexanamide derivatives with triazole moeity

    • 摘要: 为寻找高效的杀菌活性化合物,在前期十三元氮杂大环内酯化合物   Z13-5  的基础上尝试进行结构改造,保留三唑与环己甲酰胺结构,通过酰胺化及叠氮-炔烃点击反应等设计并合成了26个未见文献报道的目标化合物,其结构均通过核磁共振氢谱 (1H NMR)、碳谱 (13C NMR) 及高分辨质谱 (HRMS) 确证。初步杀菌活性测定结果表明:与化合物   Z13-5  相比,目标化合物的杀菌活性有所下降,在50 mg/L下,除化合物   7g  对辣椒疫霉病菌的抑制率可达91%外,其余化合物对供试病原真菌的抑制率均低于50%。

       

      Abstract: In order to discover novel compounds with high fungicidal activities, a series of new compounds were designed using macrocyclic compound   Z13-5   as the lead compound. And the triazole and cyclohexanamide moeities were retained. 26 new target compounds were synthesized through azidation, azic-alkyne click reaction, etc, and characterized by 1H NMR, 13C NMR and HRMS spectral data. Preliminary bioassay indicated that fungicidal activities of the target compounds were lower than compound   Z13-5  . At the concentration of 50 mg/L, the inhibition rates of most of the target compounds to the tested pathogenic fungi were less than 50%, except   7g   had 91% inbition rate to Phytophthora capsicum.

       

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