title: Design, synthesis and in vitro antibacterial activity of 7-(4-alkoxyimino-3-aminomethylpiperidin-1-yl)fluoroquinolone derivatives.
abstract: We report herein the design and synthesis of novel 7-(4-alkoxyimino-3-aminomethylpiperidin-1-yl) fluoroquinolone derivatives. The antibacterial activity of the newly synthesized compounds was evaluated and compared with gemifloxacin, levofloxacin and ciprofloxacin. Results reveal that compounds 10, 16, and 17 have good activity against all of the tested gram-positive organisms including drug-resistance strains (MICs: 0.125-4 μg/mL). In addition, compounds 16 and 17 (MICs: 4 μg/mL) were 2- to 8-fold more potent than the reference drugs against Pseudomonas aeruginosa.
authors.affiliation: Institute of Medical Biotechnology, Chinese Academy of Medical Sciences, Peking Union Medical College, Beijing 100050, China.
authors.forename: Yun
authors.initials: Y
authors.lastname: Chai
authors.forename: Jian
authors.initials: J
authors.lastname: Wang
authors.forename: Mingliang
authors.initials: M
authors.lastname: Liu
authors.forename: Hong
authors.initials: H
authors.lastname: Yi
authors.forename: Lanying
authors.initials: L
authors.lastname: Sun
authors.forename: Xuefu
authors.initials: X
authors.lastname: You
authors.forename: Huiyuan
authors.initials: H
authors.lastname: Guo
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D024841:Fluoroquinolones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D050112:Imino Pyranoses / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D011550:Pseudomonas aeruginosa / Q000187:drug effects*
chemical_list: D000900:Anti-Bacterial Agents; D024841:Fluoroquinolones; D050112:Imino Pyranoses