Multicomponent Domino Synthesis and Antibacterial Activity of Neomycin–Sugar Conjugates

This manuscript is dedicated to the memory of Vincenzo Volonterio

Abstract

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.

Key words

multicomponent reaction - domino reaction - aminoglycosides - carbodiimides - antibiotics

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