The synthesis and antibacterial activity of 2-carbolinyl-carbapenems: potent anti-MRSA/MRCNS agents

A series of 2-carbolinyl-carbapenems was prepared via the Stille stannane coupling reaction. This new class of antibiotics exhibited potent activity in vitro against methicillin-resistant Staphylococcus aureus (MRSA) and methicillin-resistant coagulase negative staphylococci (MRCNS) as well as a broad spectrum of antibacterial activity. A high resistance to the mammalian dehydropeptidase, DHP-1, was also observed.