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.
- Author:
Hui-Jie YU
1
;
Wei-Cheng ZHOU
Author Information
- Publication Type:Journal Article
- MeSH: Anti-Bacterial Agents; chemical synthesis; chemistry; pharmacology; Escherichia coli; drug effects; Fluoroquinolones; chemical synthesis; chemistry; pharmacology; Microbial Sensitivity Tests; Molecular Structure; Oxazolidinones; chemical synthesis; chemistry; pharmacology; Staphylococcus; drug effects; Structure-Activity Relationship
- From: Acta Pharmaceutica Sinica 2006;41(10):990-999
- CountryChina
- Language:Chinese
-
Abstract:
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.
