College of Chemistry and Chemical Engineering, and Biomedical Engineering Center, State Key Laboratory of Chemo/Biosensing and Chemometrics, Hunan University, Changsha 410082, China.
Eur J Med Chem. 2010 Mar;45(3):1181-8. doi: 10.1016/j.ejmech.2009.12.045. Epub 2009 Dec 28.
The synthesis and structure-activity relationships of a series of new penems bearing ferrocenyl group attached to the C-2 position of the penem nucleus were described. The beta-lactanic derivatives obtained had been characterized as sodium salts, through (1)H NMR and IR, as well as through element analysis. Their in vitro antibacterial activities against both Gram-positive including meticillin-resistant Staphylococcus aureus (MRSA) and Gram-negative bacteria were tested. Most of the penems exhibited superior or equivalent efficacy of antibacterial activity as well as high stability to renal dehydropeptidase-I (DHP-I) compared with faropenem. In particular, the compound 14h having a heterocyclic group showed the most potent antibacterial activity.
描述了一系列新型青霉素的合成及构效关系，这些青霉素的核心 C-2 位置连接有二茂铁基团。通过（1）H NMR 和 IR 以及元素分析，得到的β-内酰胺衍生物被表征为钠盐。它们对革兰氏阳性菌（包括耐甲氧西林金黄色葡萄球菌（MRSA））和革兰氏阴性菌的体外抗菌活性进行了测试。与法罗培南相比，大多数青霉素具有更好或相当的抗菌活性和对肾去氢肽酶-I（DHP-I）的高稳定性。特别是具有杂环基团的化合物 14h 表现出最强的抗菌活性。
