Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 58, Issue 12, Pages 5137-5142Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.5b00366
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- Merck and Co, Inc., Kenilworth, NJ
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Novel cyclic lipopeptides with different acyl tails were synthesized via a semisynthetic approach. Structure activity relationship studies revealed that lipophilicity, chain length, and the location of key aromatic functionalities of the tail modulated activity. The lead compound surotomycin exhibited significantly improved in vitro activity compared with daptomycin (MIC90 0.5 vs 2 mu g/mL) against Clostridium difficile including NAP1 epidemic strains. In hamster efficacy studies, surotomycin protected animals at a dose of 0.5 mg/kg, PO.
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