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新型含取代哌啶的氟喹诺酮衍生物的合成及体外抗菌活性。

Synthesis and in vitro antibacterial activity of novel fluoroquinolone derivatives containing substituted piperidines.

机构信息

Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, PR China.

出版信息

Bioorg Med Chem Lett. 2010 Sep 1;20(17):5195-8. doi: 10.1016/j.bmcl.2010.07.006. Epub 2010 Jul 8.

Abstract

We report herein the synthesis of novel 7-(4-alkoxyimino-3-aminomethyl-3-methylpiperidin-1-yl) fluoroquinolone derivatives. The antibacterial activity of the newly synthesized compounds was evaluated and correlated with their physicochemical properties. Results reveal that all of the target compounds have good potency in inhibiting the growth of Staphylococcus aureus and Staphylococcus epidermidis including MRSE (MIC: 0.125-4 microg/mL). Compounds 12, 13 are more potent than or comparable to levofloxacin against MRSA, Streptococcus pyogenes, Escherichia coli, Klebsiella pneumoniae, and Shigella sonnei. Compound 17 is more active than or comparable to levofloxacin against S. aureus including MRSA, S. epidermidis and S. pyogenes.

摘要

我们在此报告新型 7-(4-烷氧基亚氨基-3-氨甲基-3-甲基哌啶-1-基)氟喹诺酮衍生物的合成。评估了新合成化合物的抗菌活性,并将其与理化性质相关联。结果表明,所有目标化合物均对金黄色葡萄球菌和表皮葡萄球菌(包括 MRSE)的生长具有良好的抑制作用(MIC:0.125-4 μg/mL)。化合物 12、13 对 MRSA、化脓性链球菌、大肠杆菌、肺炎克雷伯菌和痢疾志贺菌的抑制作用强于或与左氧氟沙星相当。化合物 17 对金黄色葡萄球菌(包括 MRSA、表皮葡萄球菌和化脓性链球菌)的活性强于或与左氧氟沙星相当。

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