GLYCOPEPTIDE ANTIBIOTICS CONTAINING A DESMETHYLVANCOSAMINE RESIDUE, COMBINATORIAL LIBRARIES OF SAME AND METHODS OF PRODUCING SAME

摘要

A glycopeptide of the formula A1-A2-A3-A4-A5-A6-A7, in which each dash represents a covalent bond; wherein the group A1 comprises a modified or unmodified α-amino acid residue, alkyl, aryl, aralkyl, alkanoyl, aroyl, aralkanoyl, heterocyclic, heterocyclic-carbonyl, heterocyclic-alkyl, heterocyclic-alkyl-carbonyl, akylsulfonyl, arylsulfonyl, guanidinyl, carbamoyl, or xanthyl; wherein each of the groups A2 to A7 comprises a modified or unmodified α-amino acid residue, whereby (i) the group A1 is linked to an amino group on the group A2, (ii) each of the groups A2, A4 and A6 bears an aromatic side chain, which aromatic side chains are cross-linked together by two or more covalent bonds, and (iii) the group A7 bears a terminal carboxyl, ester, amide, or N-substituted amide group; and wherein one or more of the groups A1 to A7 is linked via a glycosidic bond to one or more glycosidic groups each having one or more sugar residues; wherein at least one of said sugar residues bears one or more substituents of the formula YXR; provided that: A4 is linked to a glycosidic group comprising a glucose residue substituted only by hydroxyl and/or amino groups and by attachement via a glycosidic bond to formula (II).