2. Academic Validation
  3. Glycopeptide carboxamides active against vancomycin-resistant enterococci

Glycopeptide carboxamides active against vancomycin-resistant enterococci

  • J Antibiot (Tokyo). 2003 Mar;56(3):289-95. doi: 10.7164/antibiotics.56.289.
Mark J Zweifel 1,  Nancy J Snyder,  Robin D G Cooper,  Thalia I Nicas,  Deborah L Mullen,  Thomas F Butler,  Michael J Rodriguez
Affiliations

Affiliation

  • 1 Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285, USA. [email protected]
PMID: 12760685 DOI: 10.7164/antibiotics.56.289
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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