| 樊玲玲,刘永淑,罗忠福,汤磊,李永.化学通报,2021,84(8):847-852,863. |
| 芳基肼衍生物的设计、合成及其抑菌活性研究 |
| Design, Synthesis and Antifungal Activity Evaluation of Arylhydrazine Derivatives |
| 投稿时间：2020-12-23 修订日期：2020-12-29 |
| DOI： |
| 中文关键词: 芳基肼衍生物 合成 抑菌活性 |
| 英文关键词:Arylhydrazine derivatives, Synthesis, antifungal activity |
| 基金项目:贵州省化学合成药物研发利用工程技术研究中心项目(黔科合[2016]平台人才5402)、贵州省普通高等学校药物化学工程研究中心项目(黔教合KY字[2014]219号)、国家自然科学基金项目(32060627)、贵州省科技计划项目(黔科合基础[2019]1269号,黔科合基础[2020]1Y111)和贵州医科大学学术新苗项目(19NSP075)资助 |
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| 中文摘要: |
| 为了寻找具有较高潜力的新型植物病原真菌抑制剂，本文以取代芳胺、3,3-二甲基-2-丁酮和乙酸乙酯为起始原料，采用Claisen缩合、氯代、重氮化、亲核取代等反应合成了16个新型的芳基肼类衍生物，其结构经1H NMR、13C NMR及ESI-MS确证。初步抑菌活性测试结果表明：目标化合物4d、4g和4j具有潜在的广谱性抑菌作用，其平均抑制率分别为64.7%、71.2%和67.8%，显著优于阳性对照药物噁霉灵（50.1%）和百菌清（60.0%）。构效关系研究表明：保持羰基α位氯原子不变，在芳基肼结构中引入甲基、氯、氟、三氟甲氧基等基团能有效提高其抑菌作用。此研究为基于芳基肼骨架的农用抑菌剂结构优化提供了参考。 |
| 英文摘要: |
| In order to explore novel compounds with high antifungal activity, a series of arylhydrazine derivatives were synthesized via Claisen condensation, chlorination, diazotization and nucleophilic substitution reaction, and their structures were confirmed by 1H NMR, 13C NMR and HRMS. The preliminary bioassays indicated that compounds 4d, 4g and 4j displayed potential and broad-spectrum antifungal activities, with corresponding average inhibition rates of 64.7%, 71.2% and 67.8%, which are obviously better than the commercialized fungicides hymexazol (50.1%) and chlorothalonil (60.0%). The structure-activity relationships reveal that keeping the chlorine atom at the carbonyl α-position unchanged, introduction of methyl, chlorine, fluorine and trifluoromethoxy groups on arylhydrazine scaffold can effectively improve the antifungal activity. This study provide a reference for the further structural optimization of arylhydrazine derivatives as antifungal agents. |
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