期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 49, 期 17, 页码 5273-5281出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm060732n
关键词
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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.
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