title: Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
abstract: A series of novel naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds were designed and synthesized. These derivatives were initially evaluated for their in vitro antibacterial activity and compounds 13a1, b1 were chosen for further evaluation their in vivo activity against systemic infections in mice. The results indicate that all of the target compounds have considerable in vitro antibacterial activity. In the in vivo experiments, 13b1 was found to be more effective than the parent drug gemifloxacin against the tested five strains, and especially its activity (ED(50):21.27 mg/kg) is 5.2-6.1 times more potent than gemifloxacin and ciprofloxacin against clinically important Gram-negative pathogen Pseudomonas aeruginosa.
authors.affiliation: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
authors.forename: Kai
authors.initials: K
authors.lastname: Lv
authors.forename: Ming-Liang
authors.initials: ML
authors.lastname: Liu
authors.forename: Lian-Shun
authors.initials: LS
authors.lastname: Feng
authors.forename: Lan-Ying
authors.initials: LY
authors.lastname: Sun
authors.forename: Ye-Xin
authors.initials: YX
authors.lastname: Sun
authors.forename: Zeng-Quan
authors.initials: ZQ
authors.lastname: Wei
authors.forename: Hui-Quan
authors.initials: HQ
authors.lastname: Guo
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects*; D008297:Male; D051379:Mice; D009287:Naphthyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D010091:Oximes / Q000737:chemistry*; D011759:Pyrrolidines / Q000737:chemistry*
chemical_list: D000900:Anti-Bacterial Agents; D009287:Naphthyridines; D010091:Oximes; D011759:Pyrrolidines