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Synthesis of octapeptin C4 and biological profiling against NDM-1 and polymyxin-resistant bacteria |
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| Authors: | Bernd Becker Mark S Butler Karl A Hansford Alejandra Gallardo-Godoy Alysha G Elliott Johnny X Huang David J Edwards Mark AT Blaskovich Matthew A Cooper |
| Institution: | Institute of Molecular Bioscience, University of Queensland, Brisbane 4072, Australia |
| Abstract: | 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. |
| Keywords: | Lipopeptide Colistin Drug resistance Antibiotic Natural product |
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