CHEMICAL MODIFICATION OF GLYCOPEPTIDE ANTIBIOTICS

New methods for the chemical modification of clinically important glyc opeptide antibiotics are reviewed. Special emphasis is placed on chemi cal modification of the domestic antibiotic eremomycin, which has a nu mber of advantages over the clinically used antibiotics vancomycin and teichoplanin. The most promising methods for glycopeptide modificatio n at the aromatic ring and carboxyl group of the seventh amino acid of the peptide core and also at the amino groups of the carbohydrate moi ety are discussed in detail. The structure-activity relations in a ser ies of glycopeptide derivatives are revealed. It is shown that the pre sence of lipophilic substituents of certain structures and sizes is ma ndatory for activity toward glycopeptide-resistant enterococci to be d isplayed. The possibility of dimerization and interaction of these der ivatives with membrane components of the bacterial cell wall is discus sed. The structures of the derivatives most active toward glycopeptide -resistant enterococci and meticillin-resistant staphylococci are pres ented.