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

Yun Chai; Mingliang Liu; Bo Wang; Xuefu You; Lianshun Feng; Yibin Zhang; Jue Cao; Huiyuan Guo

doi:10.1016/j.bmcl.2010.07.006

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

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

Authors

Yun Chai¹, Mingliang Liu, Bo Wang, Xuefu You, Lianshun Feng, Yibin Zhang, Jue Cao, Huiyuan Guo

Affiliation

¹ Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, PR China.

PMID: 20667731
DOI: 10.1016/j.bmcl.2010.07.006

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Anti-Bacterial Agents / chemical synthesis*
Anti-Bacterial Agents / chemistry
Anti-Bacterial Agents / pharmacology*
Fluoroquinolones / chemical synthesis*
Fluoroquinolones / chemistry
Fluoroquinolones / pharmacology*
Microbial Sensitivity Tests
Models, Molecular
Piperidines / chemistry*

Substances

Anti-Bacterial Agents
Fluoroquinolones
Piperidines