title: Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-5-amino/methylaminopiperidin-1-yl)fluoroquinolone derivatives.
abstract: We report herein the design and synthesis of novel 7-(3-alkoxyimino-5-amino/methylaminopiperidin-1-yl)fluoroquinolone derivatives based on the structures of new fluoroquinolones IMB and DZH. The antibacterial activity of these newly synthesized compounds was also evaluated and compared with gemifloxacin, ciprofloxacin, and levofloxacin. Results revealed that all of the target compounds 10-27 have good potency in inhibiting the growth of Staphylococcus aureus including MSSA (MIC: 0.125-8 μg/mL), Staphylococcus epidermidis including MRSE (MIC: 0.25-16 μg/mL), Streptococcus pneumoniae (MIC: 0.125-4 μg/mL), and Escherichia coli (MIC: 0.25-0.5 μg/mL). In particular, some compounds showed useful activity against several fluoroquinolone-resistant strains, and the most active compound 15 was found to be 16-128, 2-32, and 4-8-fold more potent than the three reference drugs against fluoroquinolone-resistant MSSA, MRSA, and MRSE.
authors.affiliation: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, PR China.
authors.forename: Yibin
authors.initials: Y
authors.lastname: Zhang
authors.forename: Guoqing
authors.initials: G
authors.lastname: Li
authors.forename: Mingliang
authors.initials: M
authors.lastname: Liu
authors.forename: Xuefu
authors.initials: X
authors.lastname: You
authors.forename: Lianshun
authors.initials: L
authors.lastname: Feng
authors.forename: Kai
authors.initials: K
authors.lastname: Lv
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; D024881:Drug Resistance, Bacterial / Q000187:drug effects; D004926:Escherichia coli / Q000187:drug effects; D024841:Fluoroquinolones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D013211:Staphylococcus aureus / Q000187:drug effects; D013212:Staphylococcus epidermidis / Q000187:drug effects; D013296:Streptococcus pneumoniae / Q000187:drug effects
chemical_list: D000900:Anti-Bacterial Agents; D024841:Fluoroquinolones