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

A novel series of mutilin 14-carbamates has been discovered as a result of structure-activity studies on the naturally occurring antibiotic pleuromuti lin (1). In particular, the 4-methoxybenzoylcarbamate, SE-222734 (15o) disp lays potent antibacterial activity against a number of bacterial pathogens which are resistant to currently used agents and shows enhanced metabolic s tability when compared to earlier pleuromutilin derivatives. Such derivativ es therefore have the potential to provide a new class of antibacterial age nts for human therapy which address the threat of bacterial resistance. (C) 2001 Elsevier Science Ltd. All rights reserved.