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  • Title: Mono and double modified teicoplanin aglycon derivatives on the amino acid no. 7; structure-activity relationship.
    Author: Pavlov AY, Preobrazhenskaya MN, Malabarba A, Ciabatti R, Colombo L.
    Journal: J Antibiot (Tokyo); 1998 Jan; 51(1):73-8. PubMed ID: 9531990.
    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.
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