Synthesis and antibacterial activities of 7-4-［2-［2-substituted-4-((5S)-5-acetylaminomethyl-2-oxo-oxazolidin-3-yl)-phenyl］-ethyl］-piperazin-1-yl-fluoroquinolones

AimTo find out new oxazolidinone-fluoroquinolone derivatives with high antibacterial activity. MethodsSome 7-4-［2-［2-substituted-4-((5S)-5- acetylaminomethyl-2-oxo-oxazolidin-3-yl)-phenyl］-ethyl］-piperazin-1-yl-fluoroquinolones were designed and synthesized, and their antibacterial activities were tested in vitro. ResultsTwenty target compounds were obtained and their structures were confirmed by ^{1H NMR and MS. The target compounds had high antibacterial activities in vitro, especially, the activity of compound 22 against Enterococcus faecium was 16-fold and 64-fold more potent than that of linezolid and norfloxacin, respectively, and its MIC value against Staphylococcus aureus was 4-fold lower than that of linezolid. ConclusionThe oxazolidinone-fluoroquinolone derivatives improved the antibacterial activities.}