The present invention provides novel glycopeptides antibiotic derivatives.
These glycopeptide antibiotic derivatives are characterized in that a sugar residue (I) represented by the formula:
(wherein n is an integer of 1 to 5; Sugs are each independently a monosaccharide, (Sug)n is a divalent sugar residue formed by binding of same or different 1 to 5 monosaccharides; RA1 is optionally substituted lower alkyl, optionally substituted lower alkenyl, or optionally substituted cycloalkyl; and RE is OH or NHAc (Ac is acetyl))
is bound to an aromatic ring of the fourth amino acid residue in the glycopeptide skeleton.
These derivatives have antibacterial activity against vancomycin-resistant bacteria.
本发明提供了新型糖肽抗生素衍
生物。
这些糖肽抗生素衍
生物的特征在于由式(I)代表的糖残基:
(其中n是1至5的整数;Sugs各自独立地是
单糖,(Sug)n是由相同或不同的1至5
单糖结合形成的二价糖残基;RA1是任选取代的低级烷基、任选取代的低级烯基或任选取代的环烷基;RE是OH或NHAc(Ac是乙酰基))
与糖肽骨架中第四个
氨基酸残基的芳香环结合。
这些衍
生物对耐
万古霉素细菌具有抗菌活性。