TRIAZOLE-BASED AMINOGLYCOSIDE-PEPTIDE CONJUGATES AND METHODS OF USE

摘要

Aminoglycoside-amino acid and -peptide conjugates comprising a triazolyl linker are provided along with efficient methods of their preparation. The aminoglycoside may be an aminoglycoside antibiotic. Conjugates comprising an aminoglycoside antibiotic may exhibit antimicrobial activities against Gram-positive and/or Gram-negative strains and display significantly enhanced activity against multi-drug resistant MRSA and MRSE when compared to their unconjugated aminoglycoside antibiotic counterparts.