title: Synthesis and in vitro antibacterial activity of gemifloxacin derivatives containing a substituted benzyloxime moiety.
abstract: A series of novel gemifloxacin (GMFX) derivatives containing a substituted benzyloxime moiety with remarkable improvement in lipophilicity were synthesized. The target compounds evaluated for their in vitro antibacterial activity against representative strains. Our results reveal that most of the target compounds have considerable potency against all of the tested gram-positive strains including MRSA and MRSE (MIC: <0.008-8 μg/mL), although they are generally less active than the references against the gram-negative strains. In particular, compound 11l (MIC: <0.008-4 μg/mL) was found to be 8-2048 and 2-128 times more potent than levofloxacin (LVFX) and GMFX against the gram-positive strains, respectively. Moreover, against MRSA clinical isolates, 11l (MIC(90): 1 μg/mL) is 8-fold more active than GMFX, and 2-fold more active than GMFX and moxifloxacin against MRSE clinical isolates (MIC(90): 4 μg/mL).
authors: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
authors: Lianshun
authors: L
authors: Feng
authors: Kai
authors: K
authors: Lv
authors: Mingliang
authors: M
authors: Liu
authors: Shuo
authors: S
authors: Wang
authors: Jing
authors: J
authors: Zhao
authors: Xuefu
authors: X
authors: You
authors: Sujie
authors: S
authors: Li
authors: Jue
authors: J
authors: Cao
authors: Huiyuan
authors: H
authors: Guo
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects*; D060326:Chemistry Techniques, Synthetic; D024841:Fluoroquinolones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000077735:Gemifloxacin; D057927:Hydrophobic and Hydrophilic Interactions; D008826:Microbial Sensitivity Tests; D009287:Naphthyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D010091:Oximes / Q000737:chemistry*
chemical_list: D000900:Anti-Bacterial Agents; D024841:Fluoroquinolones; D009287:Naphthyridines; D010091:Oximes; D000077735:Gemifloxacin