Synthesis, characterization and antibacterial activities of some new ferrocene-containing penems.

European journal of medicinal chemistry 2009 Dec 28; In press

Long B, He C, Yang Y, Xiang J

College of Chemistry and Chemical Engineering, and Biomedical Engineering Center, State Key Laboratory of Chemo/Biosensing and Chemometrics, Hunan University, Changsha, 410082, China.

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.

Keywords: antibacterial