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

被引：24

作者：

Chai, Yun

Liu, Mingliang ^{[1
]}

Wang, Bo

You, Xuefu

Feng, Lianshun

Zhang, Yibin

Cao, Jue

Guo, Huiyuan

机构：

[1] Chinese Acad Med Sci, Inst Med Biotechnol, Beijing 100050, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 17期

关键词：

Fluoroquinolone; Synthesis; Antibacterial activity;

D O I：

10.1016/j.bmcl.2010.07.006

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

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 mu g/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. (C) 2010 Elsevier Ltd. All rights reserved.

引用

收藏

页码：5195 / 5198

页数：4

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