title: Mono and double modified teicoplanin aglycon derivatives on the amino acid no. 7; structure-activity relationship.
abstract: A series of 7d-aminomethylated derivatives (mono modified) and their amides (double modified) at the amino acid No. 7 of teicoplanin aglycon were prepared with the aim of obtaining activity against vancomycin-resistant VanA enterococci. Among mono modified compounds, the 7d-n-decylaminomethyl derivative was the most active against VanA enterococci (4 micrograms/ml). Amides of the latter with 3-dimethylamino-propylamine or methylamine were found to be up to four times more active against glycopeptide-susceptible Gram-positive bacteria, and up to four times less active against VanA enterococci than the starting compound.
authors.affiliation: Institute of New Antibiotics, Russian Academy of Medical Sciences, Moscow, Russia.
authors.forename: A Y
authors.initials: AY
authors.lastname: Pavlov
authors.forename: M N
authors.initials: MN
authors.lastname: Preobrazhenskaya
authors.forename: A
authors.initials: A
authors.lastname: Malabarba
authors.forename: R
authors.initials: R
authors.lastname: Ciabatti
authors.forename: L
authors.initials: L
authors.lastname: Colombo
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D013210:Staphylococcus / Q000187:drug effects; D013291:Streptococcus / Q000187:drug effects; D013329:Structure-Activity Relationship; D017334:Teicoplanin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000900:Anti-Bacterial Agents; D017334:Teicoplanin