| 崔军军刘文陆傅磊△.四氮唑类化合物的合成及体外抑菌活性研究[J].,2012,12(18):3478-482 |
| 四氮唑类化合物的合成及体外抑菌活性研究 |
| Synthesis and Antibacterial Activity in Vitro of Tetrazoles |
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| DOI： |
| 中文关键词: 四氮唑 合成 点击化学 抑菌活性 构效关系 |
| 英文关键词: Tetrazole Synthesis Click Chemistry Antibacterial activity Structure activity relationship |
| 基金项目: |
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| 摘要点击次数: 712 |
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| 中文摘要: |
| 目的：利用点击化学反应合成四氮唑类化合物，寻找温和的反应条件。对合成的四氮唑类化合物进行体外抑菌活性研究，以
期发现抑菌活性化合物并初步研究其构效关系。方法：以氰基类化合物和叠氮钠为原料，溴化锌为催化剂，通过点击化学反应合
成一类四氮唑结构化合物并研究其合成工艺条件的优化。利用微量二倍稀释法对合成的四氮唑类化合物进行体外抑菌活性测
试。结果：利用所得到的优化点击化学反应条件合成了11 个四氮唑类化合物，并发现化合物2h 具有广谱抑菌活性。结论：优化后
的点击化学反应条件温和，后处理方便，产率较高。抑菌活性和构效关系研究为后续的四氮唑类化合物抑菌活性研究工作提供了
一定的基础。 |
| 英文摘要: |
| Objective: Synthesis of tetrazoles by click chemistry reaction and modify the reaction conditions. Investigating the antibacterial
avtivity of tetrazoles in vitro. Methods: Tetrazoles was prepared from nitriles and sodium azide as materials and catalyzed by
ZnBr2; The in vitro antibacterial activities of the synthesized tetrazoles was presented using the doubling dilution method and the SAR
was studied. Results: A mild, convenient Click reaction method was found and 11 tetrazole compounds were produced under this
method. Through an in vitro antibacterial assay, the compound 2h has a broad range of antibacterial activity. Conclusion: The optimized
click chemistry reaction conditions are mild, convenient and high yield. The result of primary antibacterial investigation and the SAR
analysis provides some basic contribution for the following study of tetrazole compound's antibacterial activity. |
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