The present invention relates to inhibitors of aminoglycoside 6'-N-acetyltransferases of Formula I: R--X--Y-Z Formula I wherein: R is selected from the group consisting of: R.sub.1 is selected from the group consisting of OH and R.sub.2 is selected from the group consisting of OH and R.sub.3 is selected from the group consisting of NH.sub.2 and OH; R.sub.4 is selected from the group consisting of NH.sub.2 and R.sub.5 is selected from the group consisting of OMe, OEt OPr, and O-iPr; X is selected from the group consisting of NH and O; Y is selected from the group consisting of: R.sub.6 is selected from the group consisting of OH, CH.sub.3, and OCH.sub.3; n is an integer ranging from 1 to 10; and Z is selected from the group consisting of: and R.sub.7 is selected from the group consisting of OH, OMe, OEt OPr, O-iPr, O-tBu and