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Chin. J. Org. Chem. ›› 2014, Vol. 34 ›› Issue (4): 829-834.DOI: 10.6023/cjoc201311027 Previous Articles     Next Articles

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新型喹啉酮类膦酸酯衍生物的合成与抗菌活性

杨家强a, 胡月维a, 谷晴a, 李明刚a, 李明强b, 宋宝安c   

  1. a 遵义医学院药学院 遵义 563003;
    b 遵义医学院微生物与免疫学实验室 遵义 563003;
    c 贵州大学精细化工研究中心 贵阳 550025
  • 收稿日期:2013-11-15 修回日期:2013-12-11 发布日期:2013-12-23
  • 通讯作者: 杨家强 E-mail:yjqcn@126.com
  • 基金资助:

    贵州省科技厅基金（No. 黔科合J字LKZ[2010]47）资助项目.

Synthesis and Antibacterial Activities of Novel Phosphonate Derivatives Containing Quinolinone Moiety

Yang Jiaqianga, Hu Yueweia, Gu Qinga, Li Mingganga, Li Mingqiangb, Song Baoanc   

  1. a School of Pharmacy, Zunyi Medical College, Zunyi 563003;
    b Laboratory of Microbiology and Immunology, Zunyi Medical College, Zunyi 563003;
    c Center for Research and Development of Fine Chemicals, Guizhou University, Guiyang 550025
  • Received:2013-11-15 Revised:2013-12-11 Published:2013-12-23
  • Supported by:

    Project supported by the Technology Department of Guizhou Province (No. LKZ[2010]47).

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According to substructure link principle, a series of novel phosphonate derivatives bearing quinolinone moiety were designed and synthesized. The structures of the products were confirmed by IR, 1H NMR and MS data. The antibacterial activities of the products against S. aureus, E.coli, drug-resistant S. aureus were evaluated by the agar dilution method. The results demonstrated that some compound exhibited superior activities against drug-resistant S. aureus compared with norfloxacin. Especially, compound Ⅲk showed more potent activities against MRSA15# with minimum inhibitory concentration (MIC) values of 6.2 mg/mL, and against QRSA7# with MIC values of 3.1 mg/mL.

Key words: quinolinone, α-aminophosphonate, amide, synthesis, antibacterial activity