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有机化学
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有机化学 ›› 2014, Vol. 34 ›› Issue (4): 829-834.DOI: 10.6023/cjoc201311027 上一篇    下一篇

研究简报

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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1188

被引次数

4 | 6

根据活性结构拼合原理，设计合成了一系列新型喹啉酮类膦酸酯衍生物，其结构经IR，1H NMR，MS及元素分析确认. 采用两倍稀释法测试目标化合物对金黄色葡萄球菌、大肠埃希菌、耐甲氧西林金葡菌、耐喹诺酮金葡菌的抑制活性，结果表明：部分目标化合物对耐药菌的抑制作用略优于对照药诺氟沙星，尤以化合物Ⅲk最好，对MRSA15#，QRSA7#的最小抑菌浓度（MIC）值分别为6.2，3.1 mg/mL.

关键词: 喹啉酮, α-氨基膦酸酯, 酰胺, 合成, 抗菌活性

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