噁唑烷酮类化合物的合成及抗菌活性  

Synthesis and antibacterial activities of new oxazolidinone derivatives

作　　者：翟鑫[1] 洪伟[1] 熊莺[1] 宫平[1] 

机构地区：[1]沈阳药科大学制药工程学院,辽宁沈阳110016

出　　处：《中国药物化学杂志》2004年第5期263-266,M003,共5页Chinese Journal of Medicinal Chemistry

摘　　要：目的设计合成唑烷酮类化合物 ,并对其体外抗菌活性进行初步评价。方法以 3,4 二氟硝基苯为原料 ,经多步反应合成目标化合物 ;采用微量液体稀释法 ,检测目标化合物对金黄色葡萄球菌和表皮葡萄球菌的抑制和杀灭作用。结果与结论合成了 10个新化合物 ,经1H NMR、MS确证其结构。体外试验表明 :化合物 7f的体外抗菌活性与对照药物利奈唑酮相当 ,化合物 7a、8c和8d表现出一定的抗菌活性。Aim To design and synthesize a ser ie s of new oxazolidinone derivatives and evaluate their antibacterial activities in vitro primarily.Method Ten target compounds were synthesized in several steps with the starting material 3,4-dif l uoronitrobenzene and their antibacterial activities in vitro against Strap hylococcus aureus and Straphylococcus epidermidis were examined respective ly.R esults and conclusion The structures of the ten new compounds were confi rmed by 1H-NMR and MS.Pharmacological tests showed that compound 7f has the same potent antibacterial activity as that of the c ontrol drug linezolid and compoun ds 7a,8c and 8d also have some a ntibacterial activities.

关 键 词：药物化学 制备 化学合成 噁唑烷酮类化合物 利奈唑酮 抗菌活性 

分 类 号：R914[医药卫生—药物化学] R96[医药卫生—药学]