Synthesis of Hydrophobic TV'-Mono and 7V'57V"-Doiible Alkylated Eremomycins Inhibiting the Transglycosylation Stage of Bacterial Cell Wall Biosynthesis

A series of hydrophobic TV7-monoand A^iV'-double alkylated derivatives of the glycopeptide antibiotic eremomycin were synthesized by reductive alkylation after preliminary protection of the TV-terminal amino group of the peptide backbone. The investigation of the antibacterial activity in vitro showed that Af'-C10H21-and A^'-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

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