7-4-［2-［2-取代-4-((5<i>S</i>)-5-乙酰胺甲基-2-氧代-噁唑烷-3-基)苯基］乙基］哌嗪-1-基-氟喹诺酮类化合物的合成与抗菌活性

7-4-［2-［2-取代-4-((5S)-5-乙酰胺甲基-2-氧代-噁唑烷-3-基)苯基］乙基］哌嗪-1-基-氟喹诺酮类化合物的合成与抗菌活性

摘要: 目的寻找新型的噁唑烷酮-氟喹诺酮类抗菌药物。方法设计合成了7-4-［2-［2-取代-4-((5S)-5-乙酰胺甲基-2-氧代-噁唑烷-3-基)苯基］乙基］哌嗪-1-基-氟喹诺酮类化合物，测定其体外抗菌活性。结果共合成20个目标化合物，经^{1^{H NMR和MS确证结构。目标化合物具有较好的体外抗菌活性，尤其是化合物22，对屎肠球菌的抑制活性分别是吗啉噁酮和诺氟沙星的16倍和64倍，对金葡菌的抑制活性为吗啉噁酮的4倍。结论某些带有氟喹诺酮结构片段的噁唑烷酮类化合物抗菌活性加强。}}

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 ^{1^{H 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.}}