title: Glycopeptide carboxamides active against vancomycin-resistant enterococci.
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.
authors.affiliation: Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285, USA. ZWEIFEL_MARK_J@LILLY.COM
authors.forename: Mark J
authors.initials: MJ
authors.lastname: Zweifel
authors.forename: Nancy J
authors.initials: NJ
authors.lastname: Snyder
authors.forename: Robin D G
authors.initials: RD
authors.lastname: Cooper
authors.forename: Thalia I
authors.initials: TI
authors.lastname: Nicas
authors.forename: Deborah L
authors.initials: DL
authors.lastname: Mullen
authors.forename: Thomas F
authors.initials: TF
authors.lastname: Butler
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Rodriguez
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D016983:Enterococcus / Q000187:drug effects*; D006020:Glycopeptides; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D016339:Spectrometry, Mass, Fast Atom Bombardment; D013329:Structure-Activity Relationship; D020713:Vancomycin Resistance
chemical_list: D000900:Anti-Bacterial Agents; D006020:Glycopeptides