Synthesis and bioactivity of fused- and spiro-β-lactone-lactam systems

Abstract

An investigation of the formation of fused- and spiro-β-lactone annulate to γ-lactams has shown that the fused systems are formed preferentially, under standard conditions, but that spiro systems are accessible only when the formation of the fused system is blocked and require careful optimisation of reaction conditions. These systems display both weak antibacterial activity and proteasome inhibition.