MONO AND DOUBLE MODIFIED TEICOPLANIN AGLYCON DERIVATIVES ON THE AMINO-ACID NO.-7 - STRUCTURE-ACTIVITY RELATIONSHIP

A series of 7d-aminomethylated derivatives (mono modified) and their a mides (double modified) at the amino acid No. 7 of teicoplanin aglycon were prepared with the aim of obtaining activity against vancomycin-r esistant VanA enterococci. Among mono modified compounds, the 7d-n-dec ylaminomethyl derivative was the most active against VanA enterococci (4 mu g/ml). Amides of the latter with 3-dimethylamino-propylamine or methylamine were found to be up to four times more active against glyc opeptide-susceptible Gram-positive bacteria, and up to four times less active against VanA enterococci than the starting compound.