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有机化学
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有机化学 ›› 2010, Vol. 30 ›› Issue (12): 1840-1847. 上一篇    下一篇

研究论文

青霉烯二茂铁衍生物的合成与抗菌活性研究

杨迎宾1，何纯莲2，吴超1，刘开建1，向建南*,1,3,4   

  1. (1湖南大学化学化工学院 长沙 410082)
    (2湖南师范大学医学院 长沙 410081)
    (3湖南大学生物医学工程中心 长沙 410082)
    (4湖南大学化学生物传感与化学计量学国家重点实验室 长沙 410082)
  • 收稿日期:2009-12-29 修回日期:2010-05-11 发布日期:2010-07-05
  • 通讯作者: 向建南 E-mail:jnxiang@hnu.cn
  • 基金资助:

    湖南省自然科学基金;长沙市自然科学基金

Synthesis and Antibacterial Activities of Penem Ferrocene Deriva-tives

Yang Yingbin1 He Chunlian2 Wu Chao1 Liu Kaijian1 Xiang Jian-nan*,1,3,4   

  1. (1 College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082)
    (2 College of Medicine, Hunan Normal University, Changsha 410081)
    (3 Biomedical Engineering Center, Hunan University, Changsha 410082)
    (4 State Key Laboratory of Chemo/Biosensing and Chemometrics, Hunan Univer-sity, Changsha 410082)
  • Received:2009-12-29 Revised:2010-05-11 Published:2010-07-05
  • Contact: XIANG Jian-Nan E-mail:jnxiang@hnu.cn
  • Supported by:

    Natural Science Foundation of Hunan Province;Science and Technology Foundation of Changsha

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被引次数

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为了探寻更具活性的青霉烯类抗生素, 设计并合成了8个新的青霉烯二茂铁衍生物, 并进行了结构表征与确认. 采用琼脂平皿二倍稀释法测定了它们和法罗培南对金黄色葡萄球菌等菌种的最小抑菌浓度(MIC), 并对此类化合物的构效关系进行了探讨. 结果显示, C-2位被二茂铁基团取代的青霉烯类化合物的抗菌活性优于法罗培南或与其相当, 尤其是含有杂环取代基的化合物8h抗菌活性显著.

关键词: 青霉烯, 二茂铁衍生物, 合成, 抗菌活性, 构效关系

In order to enhance the antibacterial activities of penems antibiotics, eight novel penem ferrocene derivatives were synthesized and their structures were characterized. The minimal inhibitory concentration (MIC) of these compounds and farropenem against Staphylococcus aureus etc. was determined by the agar dilution method. The structure-activity relationships of these compounds were also discussed. Results showed that penems of which the C-2 position modified by ferrocene groups exhibited superior or equivalent antibacterial activities compared with faropenem. In particular, compound 8h having a heterocyclic group showed the most potent antibacterial activities.

Key words: penem, ferrocene derivative, antibacterial activity, synthesis, structure-activity relationship