title: Synthesis and in vitro antibacterial activity of novel fluoroquinolone derivatives containing substituted piperidines.
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.
authors.affiliation: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, PR China.
authors.forename: Yun
authors.initials: Y
authors.lastname: Chai
authors.forename: Mingliang
authors.initials: M
authors.lastname: Liu
authors.forename: Bo
authors.initials: B
authors.lastname: Wang
authors.forename: Xuefu
authors.initials: X
authors.lastname: You
authors.forename: Lianshun
authors.initials: L
authors.lastname: Feng
authors.forename: Yibin
authors.initials: Y
authors.lastname: Zhang
authors.forename: Jue
authors.initials: J
authors.lastname: Cao
authors.forename: Huiyuan
authors.initials: H
authors.lastname: Guo
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D024841:Fluoroquinolones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D010880:Piperidines / Q000737:chemistry*
chemical_list: D000900:Anti-Bacterial Agents; D024841:Fluoroquinolones; D010880:Piperidines