Semi-synthetic glycopeptides having antibacterial activity are based on
modifications of the eremomycin, A82846B, vancomycin, teicoplanin, and
A-40,926 scaffolds, in particular, acylation of the sugar moieties on
these scaffolds with certain acyl groups; and/or conversion of an acid
moiety on the macrocyclic ring of these scaffolds to certain substituted
amides; or having a combination of an alkylation modification of the
amino substituent on the amino-substituted sugar moiety on these
scaffolds with certain alkyl groups or acylation modification of the
amino substituent on the amino-substituted sugar moiety on this scaffold
with certain alkyl groups, and conversion of the acid moiety on the
macrocyclic ring of this scaffolds to certain substituted amides. Also
provided are methods for the synthesis of the compounds, pharmaceutical
compositions containing the compounds, and methods of use of the
compounds for the treatment and/or prophylaxis of diseases, especially
bacterial infections.