Pleuromutilins. Part 1. The identification of novel mutilin 14-carbamates |
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Authors: | Brooks G Burgess W Colthurst D Hinks J D Hunt E Pearson M J Shea B Takle A K Wilson J M Woodnutt G |
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Institution: | SmithKline Beecham Pharmaceuticals Research and Development, Discovery Chemistry Europe, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK |
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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. |
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