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 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.
Pavlov
A Y
AY
Institute of New Antibiotics, Russian Academy of Medical Sciences, Moscow, Russia.
Preobrazhenskaya
M N
MN
Malabarba
A
A
Ciabatti
R
R
Colombo
L
L
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
D000900:Anti-Bacterial Agents; D017334:Teicoplanin