Synthesis of octapeptin C4 and biological profiling against NDM-1 and polymyxin-resistant bacteria. Issue 11 (1st June 2017)

• Record Type: Journal Article
• Authors: Becker, Bernd; Butler, Mark S.; Hansford, Karl A.; Gallardo-Godoy, Alejandra; Elliott, Alysha G.; Huang, Johnny X.; Edwards, David J.; Blaskovich, Mark A.T.; Cooper, Matthew A.
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 27:Issue 11(2017)
• Page Start: 2407
• Page End: 2409
• Publication Date: 2017-06-01
• Subjects: Lipopeptide -- Colistin -- Drug resistance -- Antibiotic -- Natural product; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2017.04.027
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: 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.