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


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.

SUBMITTER: Becker B 

PROVIDER: S-EPMC5515593 | biostudies-literature | 2017 Jun

REPOSITORIES: biostudies-literature

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

Becker Bernd B   Butler Mark S MS   Hansford Karl A KA   Gallardo-Godoy Alejandra A   Elliott Alysha G AG   Huang Johnny X JX   Edwards David J DJ   Blaskovich Mark A T MAT   Cooper Matthew A MA  

Bioorganic & medicinal chemistry letters 20170412 11


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. ...[more]

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