910127-07-0Relevant academic research and scientific papers
Synthesis and structure-activity relationships of truncated bisubstrate inhibitors of aminoglycoside 6′-N-acetyltransferases
Gao, Feng,Yan, Xuxu,Shakya, Tushar,Baettig, Oliver M.,Ait-Mohand-Brunet, Samia,Berghuis, Albert M.,Wright, Gerard D.,Auclair, Karine
, p. 5273 - 5281 (2007/10/03)
Truncated aminoglycoside-coenzyme A bisubstrate analogues were efficiently prepared using a convergent approach where the amine and the thiol are coupled in one pot with the addition of a linker, without the need for protecting groups. These derivatives were tested for their effect on the activity of the resistance-causing enzyme aminoglycoside 6′-N-acetyltransferase Ii, and key structure-activity relationships are reported. Moreover, one of the inhibitors is able to block aminoglycoside resistance in cells expressing this enzyme.
Inhibitors of aminoglycoside 6'-N-acetyltransferases, compositions and uses thereof
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Page/Page column 17, (2008/06/13)
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: R1 is selected from the group consisting of OH and R2 is selected from the group consisting of OH and R3 is selected from the group consisting of NH2 and OH; R4 is selected from the group consisting of NH2 and R5 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: R6 is selected from the group consisting of OH, CH3, and OCH3; n is an integer ranging from 1 to 10; and Z is selected from the group consisting of: and R7 is selected from the group consisting of OH, OMe, OEt OPr, O-iPr, O-tBu and
