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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 search for more active penem antibiotics, eight novel penicillin ferrocene derivatives were designed and synthesized, and their structures were characterized and confirmed.And they were compared with faropenem by two-fold agar dilution On the minimum inhibitory concentration (MIC) of Staphylococcus aureus and other species, and the structure-activity relationship of these compounds was discussed.The results showed that the C-2 position was ferrocene group substituted penem compounds The antimicrobial activity of faropenem is superior to or comparable to that of faropenem, especially 8h with heterocyclic substituents.