| Autor: |
Pavlov AY; Institute of New Antibiotics of the Russian Academy of Medical Sciences, Moscow., Miroshnikova OV, Printsevskaya SS, Olsufyeva EN, Preobrazhenskaya MN, Goldman RC, Branstrom AA, Baizman ER, Longley CB |
| Jazyk: |
angličtina |
| Zdroj: |
The Journal of antibiotics [J Antibiot (Tokyo)] 2001 May; Vol. 54 (5), pp. 455-9. |
| DOI: |
10.7164/antibiotics.54.455 |
| Abstrakt: |
A series of hydrophobic N'-mono and N',N"-double alkylated derivatives of the glycopeptide antibiotic eremomycin were synthesized by reductive alkylation after preliminary protection of the N-terminal amino group of the peptide backbone. The investigation of the antibacterial activity in vitro showed that N'-C10H21- and N'-p-(p-chlorophenyl)benzyl derivatives of eremomycin are the most active against vancomycin-resistant enterococci among the compounds obtained though they are less effective than the corresponding lipophilic derivatives of vancomycin. The introduction of two hydrophobic substituents led to a decrease in activity against both susceptible and resistant bacteria. The biochemical evaluation of the mode of action revealed that in addition to binding to D-Ala-D-Ala these compounds also have an alternative mechanism of action that does not require substrate binding. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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