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Identification of synthetic compounds active against VRE: the role of the lipidated aminoglucose and the structure of glycopeptide binding pocket.

作者信息

Jia Yanxing, Gonzalez-Zamora Eduardo, Ma Nianchun, Liu Zuosheng, Bois-Choussy Michèle, Malabarba Adriano, Brunati Cristina, Zhu Jieping

机构信息

Institut de Chimie des Substances Naturelles, CNRS, 91198 Gif-sur-Yvette Cedex, France.

出版信息

Bioorg Med Chem Lett. 2005 Oct 15;15(20):4594-9. doi: 10.1016/j.bmcl.2005.06.098.

DOI:10.1016/j.bmcl.2005.06.098
PMID:16099650
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.

摘要

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