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J Antibiot (Tokyo). 2003 Mar;56(3):289-95.

Glycopeptide carboxamides active against vancomycin-resistant enterococci.

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Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285, USA. ZWEIFEL_MARK_J@LILLY.COM


Glycopeptide antibiotics were synthesized via the PyBOP mediated condensation of aliphatic, heterocyclic and aromatic amines with the C-terminus of vancomycin, LY264826 (A82846B) and semi-synthetic derivatives of these natural products. Amides of LY264826 and vancomycin demonstrated excellent activity against staphylococci and streptococci as compared to the parent natural product. However, the amides of N-alkylated LY264826 and N-alkylated vancomycin were active against vancomycin-resistant enterococci as well as other gram-positive pathogens such as Staphylococcus aureus, S. haemolyticus, S. epidermidis and Streptococcus pneumoniae.

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