title: Identification of synthetic compounds active against VRE: the role of the lipidated aminoglucose and the structure of glycopeptide binding pocket.
abstract: A modified vancomycin binding pocket (D-O-E ring) incorporating an alpha-hydroxy-beta-amino acid at the AA4 position is designed and synthesized. Some of these compounds display potent bioactivities against both sensitive- and resistant-strains (8 microg/ml against VREF). Both the lipidated aminoglucose and the structure of the 16-membered macrocycle are found to be important for the anti-VRE activities. The polyamine appendage at the C-terminal, on the other hand, improved the activity against vancomycin-sensitive strains.
authors.affiliation: Institut de Chimie des Substances Naturelles, CNRS, 91198 Gif-sur-Yvette Cedex, France.
authors.forename: Yanxing
authors.initials: Y
authors.lastname: Jia
authors.forename: Eduardo
authors.initials: E
authors.lastname: Gonzalez-Zamora
authors.forename: Nianchun
authors.initials: N
authors.lastname: Ma
authors.forename: Zuosheng
authors.initials: Z
authors.lastname: Liu
authors.forename: Michèle
authors.initials: M
authors.lastname: Bois-Choussy
authors.forename: Adriano
authors.initials: A
authors.lastname: Malabarba
authors.forename: Cristina
authors.initials: C
authors.lastname: Brunati
authors.forename: Jieping
authors.initials: J
authors.lastname: Zhu
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D002240:Carbohydrate Sequence; D016983:Enterococcus / Q000737:chemistry / Q000187:drug effects*; D006020:Glycopeptides / Q000737:chemistry / Q000378:metabolism*; D006860:Hydrogen Bonding; D008055:Lipids / Q000737:chemistry*; D008969:Molecular Sequence Data; D011487:Protein Conformation; D020713:Vancomycin Resistance
chemical_list: D000900:Anti-Bacterial Agents; D006020:Glycopeptides; D008055:Lipids