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

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 β-lactanic derivatives obtained had been characterized as sodium salts, through 1H 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.

Graphical abstractA series of new ferrocene-containing penems had been synthesized. The results of bioassay showed that these compounds exhibited potent antibacterial activities and high stability to DHP-I.Figure optionsDownload full-size imageDownload as PowerPoint slide