910126-99-7Relevant academic research and scientific papers
PANTETHEINE DERIVATIVES AND USES THEREOF
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, (2020/06/19)
The present disclosure relates to compounds of Formula (I), (II), or (II'): (I), (II), (II'), and pharmaceutically acceptable salts or solvates thereof. The present disclosure also relates to pharmaceutical compositions comprising the compounds and therapeutic and diagnostic uses of the compounds and pharmaceutical compositions.
Inhibitors of aminoglycoside 6'-N-acetyltransferases, compositions and uses thereof
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Page/Page column 14, (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
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.
