Synthesis of octapeptin C4 and biological profiling against NDM-1 and polymyxin-resistant bacteria

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:27

Article

Becker, Bernd¹  Butler, Mark S.¹  Hansford, Karl A.¹  Gallardo-Godoy, Alejandra¹  Elliott, Alysha G.¹  Huang, Johnny X.¹  Edwards, David J.¹  Blaskovich, Mark A. T.¹  Cooper, Matthew A.¹ 

[1] Univ Queensland, Inst Mol Biosci, Brisbane, Qld 4072, Australia

关键词: Lipopeptide;    Colistin;    Drug resistance;    Antibiotic;    Natural product;   

DOI  :  10.1016/j.bmcl.2017.04.027

来源: Elsevier

【 摘 要 】

The first synthesis of octapeptin C4 was achieved using a combination of solid phase synthesis and off resin cyclisation. Octapeptin C4 displayed antibiotic activity against multi-drug resistant, NDM-1 and polymyxin-resistant Gram-negative bacteria, with moderate activity against Staphylococcus aureus. The linear analogue of octapeptin C4 was also prepared, which showed reduced activity. (C) 2017 The Authors. Published by Elsevier Ltd.

【 授权许可】

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