Provided herein are semi-synthetic glycopeptides having antibacterial activity. The semi-synthetic glycopeptides described herein are made by chemical modification of a glycopeptide by hydrolyzing the disaccharide moiety of the amino acid-4 of the parent glycopeptide in acidic medium to give the amino acid-4 monosaccharide conversion of the monosaccharide to the amino-sugar derivative acylation of the amino substituent on the amino acid-4 amino-substituted sugar moiety with certain acyl groups conversion of the amide group in amino acid-3 to various acylamide, acylsulfonamide, acylsulfonylurea derivatives aminomethylation with substituent containing sulfonamide or acylsulfonamide group on amino acid-7 through Mannich reaction and conversion of the acid moiety on the macrocyclic ring to certain substituted amides. Also provided herein are pharmaceutical compositions comprising the semi-synthetic glycopeptides, and methods of use of the semi-synthetic glycopeptides for the treatment and/or prophylaxis of diseases, especially bacterial infections.
