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, 56 (3), 289-95

Glycopeptide Carboxamides Active Against Vancomycin-Resistant Enterococci

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Glycopeptide Carboxamides Active Against Vancomycin-Resistant Enterococci

Mark J Zweifel et al. J Antibiot (Tokyo).

Abstract

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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