[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].
OBJECTIVE
To find out new oxazolidinone-fluoroquinolone derivatives with high antibacterial activity.


METHODS
Some 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.


RESULTS
Twenty 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.


CONCLUSIONS
The oxazolidinone-fluoroquinolone derivatives improved the antibacterial activities.
Yu
Hui-Jie
HJ
Shanghai Institute of Pharmaceutical Industry, Shanghai 200437, China.
Zhou
Wei-Cheng
WC
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004926:Escherichia coli / Q000187:drug effects; D024841:Fluoroquinolones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D023303:Oxazolidinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013210:Staphylococcus / Q000187:drug effects; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D024841:Fluoroquinolones; D023303:Oxazolidinones