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  

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

作　　者：于慧杰[1] 周伟澄[1] 

机构地区：[1]上海医药工业研究院,上海200437

出　　处：《药学学报》2006年第10期990-999,共10页Acta Pharmaceutica Sinica

基　　金：上海市科委资助项目(04JC14068;04DZ05902).

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1H 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。Aim 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 Enterococcusfaecium 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. Conclusion The oxazolidinone-fluoroquinolone derivatives improved the antibacterial activities.

关 键 词：氟喹诺酮 嘿唑烷酮 抗菌活性 

分 类 号：R916.2[医药卫生—药学] R916.695