Multicomponent Domino Synthesis and Antibacterial Activity of Neomycin-Sugar Conjugates

An efficient multicomponent domino process that works under mild conditions was used for the synthesis of systematically modified neomycin-sugar conjugates. The final aminoglycoside derivatives were tested against methicillin-resistant Staphylococcus aureus, Klebsiella, and E. coli strains, and show activity comparable to the parent antibiotics. Such a strategy can impact multicomponent combinatorial syntheses of diverse biologically active conjugates.