title: Antibacterial activity of G6-quaternary ammonium derivatives of a lipophilic vancomycin analogue.
abstract: A series of G6-amino derivatives of a lipophilic vancomycin analogue was prepared. Antibacterial activity of the analogues was inversely proportional to the degree of substitution of the G6-nitrogen. The fully substituted (quaternary) analogues were essentially inactive against vanA phenotype VREF strains but retained substantial activity against other bacteria, a profile reminiscent of teicoplanin.
authors.affiliation: Merck Research Laboratories, RY800-B116, PO Box 2000, Rahway, NJ 07065, USA. tim_blizzard@merck.com
authors.forename: Timothy A
authors.initials: TA
authors.lastname: Blizzard
authors.forename: Ronald M
authors.initials: RM
authors.lastname: Kim
authors.forename: Jerry D
authors.initials: JD
authors.lastname: Morgan
authors.forename: Jiang
authors.initials: J
authors.lastname: Chang
authors.forename: Joyce
authors.initials: J
authors.lastname: Kohler
authors.forename: Ruth
authors.initials: R
authors.lastname: Kilburn
authors.forename: Kevin
authors.initials: K
authors.lastname: Chapman
authors.forename: Milton L
authors.initials: ML
authors.lastname: Hammond
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004351:Drug Resistance; D057927:Hydrophobic and Hydrophilic Interactions; D008826:Microbial Sensitivity Tests; D000644:Quaternary Ammonium Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013211:Staphylococcus aureus / Q000187:drug effects; D013291:Streptococcus / Q000187:drug effects; D013329:Structure-Activity Relationship; D014640:Vancomycin / Q000031:analogs & derivatives*
chemical_list: D000900:Anti-Bacterial Agents; D000644:Quaternary Ammonium Compounds; D014640:Vancomycin