910866-19-2Relevant 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 (2006)
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.
