Jia, YanxingGonzalez-Zamora, EduardoMa, NianchunLiu, ZuoshengBois-Choussy, MicheleMalabarba, AdrianoBrunati, CristinaZhu, Jieping2010-11-252010-11-252010-11-25200510.1016/j.bmcl.2005.06.098https://infoscience.epfl.ch/handle/20.500.14299/58464A 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 compds. display potent bioactivities against both sensitive- and resistant-strains (8 micro g/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. [on SciFinder (R)]Structure-activity relationship (bactericidal; role of lipidated aminoglucose and structure of glycopeptide binding pocket in synthetic compds. active against VRE); Antibacterial agents; Staphylococcus aureus (role of lipidated aminoglucose and structure of glycopeptide binding pocket in synthetic compds. active against VRE); Glycopeptides Role: PAC (Pharmacological activity)SPN (Synthetic preparation)THU (Therapeutic use)BIOL (Biological study)PREP (Preparation)USES (Uses) (role of lipidated aminoglucose and structure of glycopeptide binding pocket in synthetic compds. active against VRE)glycopeptide vancomycin analog prepn structure activity VREtext::journal::journal article::research article