Synthesis and antibacterial activity of lipophilic carbapenems with anti-MRSA activity

A series of sulphur-linked and carbon-linked lipophilic carbapenems has been prepared and evaluated for antibacterial activity in vitro and in vivo and for affinity for PBP2′ of Staphylococcus aureus. Potent activity in vitro against methicillin-resistant S. aureus and methicillin-resistant coagulase negative staphylococci was observed despite IC50 values for PBP2′ being higher than the MIC.