Aminoglycoside–coenzyme A conjugates are challenging synthetic targets because of the wealth of functional groups and high polarity of the starting materials. We previously reported a one-pot synthesis of amide-linked aminoglycoside–CoA bisubstrates. These molecules are nanomolar inhibitors of aminoglycoside N-6′-acetyltransferase Ii (AAC (6′)- Ii), an important enzyme involved in bacterial resistance to aminoglycoside antibiotics. We ...
