| 含肟酯的吡唑衍生物的合成及其抑菌活性 |
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| 引用本文： | 沈安泽,胡恩畅,刘函如,王宇佳,王勇,马志卿,冯俊涛,雷鹏.含肟酯的吡唑衍生物的合成及其抑菌活性[J].农药学学报,2021,23(1):69-75. |
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| 作者姓名： | 沈安泽 胡恩畅 刘函如 王宇佳 王勇 马志卿 冯俊涛 雷鹏 |
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| 作者单位： | 西北农林科技大学 植物保护学院 陕西 杨凌 712100 |
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| 基金项目： | 西北农林科技大学科研启动费 (00200- Z109021809)；省级大学生创新创业训练计划项目 (S201910712256) |
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| 摘 要： | 为发现高抑菌活性的先导化合物, 结合本课题组前期研究, 设计并合成了17个新型含肟酯的吡唑衍生物, 结构经 1H NMR、13C NMR及高分辨质谱分析确证, 化合物 7q 的结构经单晶衍射确证。抑菌活性测定结果表明, 目标化合物在50 μg/mL下对苹果树腐烂病菌Valsa mali、油菜菌核病菌Sclerotinia sclerotiorum、番茄灰霉病菌Botrytis cinerea和小麦全蚀病菌Gaeumannomyces graminis均表现出一定的抑制活性, 其中化合物 7q 对番茄灰霉病菌的抑制活性较好, EC50值为7.04 μg/mL, 优于先导化合物 L1 和肟菌酯。
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| 关 键 词： | 肟酯 吡唑衍生物 合成 抑菌活性 |
| 收稿时间： | 2020-08-12 |
Synthesis and antifungal activities of pyrazole derivatives containing oxime esters |
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| Institution: | College of Plant Protection, Northwest A&F University, Yangling 712100, Shaanxi Province, China |
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| Abstract: | In order to discover lead compound with high antifungal activities, 17 novel pyrazole derivatives containing oxime esters were designed and synthesized based on our previous studies. Their structures were characterized by 1H NMR, 13C NMR and HRMS, and the crystal structure of compound 7q was confirmed by X-ray diffraction. The bioassay results showed that target compounds displayed antifungal activities against Valsa mali, Sclerotinia sclerotiorum, Botrytis cinerea and Gaeumannomyces graminis. Especially, compound 7q exhibited satisfied activity against B. cinerea with the EC50 value of 7.04 μg/mL, which was better than that of the lead compound ( L1 ) and trifloxystrobin. |
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