| 含三唑结构的环己甲酰胺衍生物的合成及杀菌活性 |
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| 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. |
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| 作者姓名： | 杜琳 张斌 宁磊 王思敏 路慧哲 张建军 董燕红 |
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| 作者单位： | 中国农业大学 理学院,北京 100193;中国林业科学研究院,北京 100091 |
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| 基金项目： | 国家自然科学基金 (31272075) |
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| 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%。
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| 关 键 词： | 三唑 环己甲酰胺 酰胺化 点击反应 杀菌活性 |
| 收稿时间： | 2019-11-01 |
Synthesis and fungicidal activity of cyclohexanamide derivatives with triazole moeity |
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| Institution: | 1.College of Science, China Agricutural Universiy, Beijing 100193, China2.Chinese Academy of Forestry Sciences, Beijing 100091, China |
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| 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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