Pleuromutilins. Part 1. The identification of novel mutilin 14-carbamates.

Abstract A novel series of mutilin 14-carbamates has been discovered as a result of structure–activity studies on the naturally occurring antibiotic pleuromutilin ( 1 ). In particular, the 4-methoxybenzoylcarbamate, SB-222734 ( 15o ) displays potent antibacterial activity against a number of bacterial pathogens which are resistant to currently used agents and shows enhanced metabolic stability when compared to earlier pleuromutilin derivatives. Such derivatives therefore have the potential to provide a new class of antibacterial agents for human therapy which address the threat of bacterial resistance.