Novel dithiocarbamate carbapenems with anti-MRSA activity

Abstract A new series of 1β-methyl carbapenems, in which a disubstituted-aminothiocarbonylthio moiety was attached to the C-2 position of the carbapenem nucleus, were prepared and evaluated for anti-MRSA activity. These derivatives showed good in vitro antibacterial activity against high-level MRSA, and the finding of good affinity for PBP-2′ supported these results. Some of the compounds having favorable protein-binding affinity showed excellent in vivo anti-MRSA activity.