Role of the glycopeptide framework in the antibacterial activity of hydrophobic derivatives of glycopeptide antibiotics |
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| Authors: | Printsevskaya Svetlana S Pavlov Andrey Y Olsufyeva Evgenia N Mirchink Elena P Preobrazhenskaya Maria N |
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| Affiliation: | Gause Institute of New Antibiotics, Russian Academy of Medical Sciences, B. Pirogovskaya 11, Moscow 119021, Russia. |
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| Abstract: | The antibacterial properties of glycopeptide antibiotics are based on their interaction with the d-Ala-d-Ala containing pentapeptide of bacterial peptidoglycan. The hydrophobic amides of vancomycin (1), teicoplanin (2), teicoplanin aglycon (3), and eremomycin (4) were compared with similar amides of minimally or low active des-(N-methyl-d-leucyl)eremomycin (5), eremomycin aglycon (6), des-(N-methyl-d-leucyl)eremomycin aglycon (7), and a teicoplanin degradation product TB-TPA (8). All hydrophobic amides of 1, 3, 4, and 6 were almost equally active against glycopeptide-resistant enterococci (GRE) minimum inhibitory concentrations (MIC)
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