青霉烯二茂铁衍生物的合成与抗菌活性研究  

Synthesis and Antibacterial Activities of Penem Ferrocene Derivatives

作　　者：杨迎宾[1] 何纯莲[2] 吴超[1] 刘开建[1] 向建南[1,3,4] 

机构地区：[1]湖南大学化学化工学院,长沙410082 [2]湖南师范大学医学院,长沙410081 [3]湖南大学生物医学工程中心,长沙410082 [4]湖南大学化学生物传感与化学计量学国家重点实验室,长沙410082

出　　处：《有机化学》2010年第12期1840-1847,共8页Chinese Journal of Organic Chemistry

基　　金：湖南省自然科学基金(No2009WK4005);长沙市自然科学基金(NoK0802152-31)资助项目

摘　　要：为了探寻更具活性的青霉烯类抗生素,设计并合成了8个新的青霉烯二茂铁衍生物,并进行了结构表征与确认.采用琼脂平皿二倍稀释法测定了它们和法罗培南对金黄色葡萄球菌等菌种的最小抑菌浓度(MIC),并对此类化合物的构效关系进行了探讨.结果显示,C-2位被二茂铁基团取代的青霉烯类化合物的抗菌活性优于法罗培南或与其相当,尤其是含有杂环取代基的化合物8h抗菌活性显著.In order to enhance the antibacterial activities of penems antibiotics, eight novel penem ferro-cene derivatives were synthesized and their structures were characterized. The minimal inhibitory concentra-tion （MIC） of these compounds and farropenem against Staphylococcus aureus etc. was determined by the agar dilution method. The structure-activity relationships of these compounds were also discussed. Results showed that penems of which the C-2 position modified by ferrocene groups exhibited superior or equivalent antibacterial activities compared with faropenem. In particular, compound 8h having a heterocyclic group showed the most potent antibacterial activities.

关 键 词：青霉烯 二茂铁衍生物 合成 抗菌活性 构效关系 

分 类 号：TQ460.1[化学工程—制药化工]