Hybrid Antibiotics Based on Azithromycin and Glycopeptides: Synthesis and Antibacterial Activity

Abstract

A series of hybrid antibiotics on the basis of azithromycin and glycopeptides with the glycopeptide molecule attached via the aminoalkylcarbamoyl spacer to 11-position of the macrolide was synthesized. All the synthesized compounds demonstrated equal or superior to azithromycin and vancomycin antibacterial activity against 7 tested strains of grampositive bacteria. The new hybrid antibiotics were more active than azithromycin or vancomycin against S.pneumoniae ATCC 49619. Some of the compounds were active against E.faecium and E.faecalis strains resistant to vancomycin.

Keywords

• vancomycin
• eremomycin
• teicoplanin aglycon
• azithromycin
• hybrid antibiotics
• antibacterial activity