A new type of chemical modification of glycopeptides antibiotics: Aminomethylated derivatives of eremomycin and their antibacterial activity

Abstract

A series of derivatives of eremomycin aminomethylated at the 7d position of the resorcinol ring of the amino acid No. 7 was prepared by interaction of eremomycin with formaldehyde and various primary and secondary amines and ammonia. The most active compound obtained was 7d-decylaminomethyl derivative, whose minimal inhibitory concentrations for clinical isolates of staphylococci are 2 ~ 8 times lower than those of the parent antibiotic. 7d-Decylaminormethyl derivative was also active against vancomycin-resistant VanA enterococci (8 μg/ml) and Neisseria gonorrhoeae (16 μg/ml).