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Your search keyword '"Baettig, Oliver M."' showing total 6 results
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5. Synthesis and structure-activity relationships of truncated bisubstrate inhibitors of aminoglycoside 6'-N-acetyltransferases.

Author

Gao F, Yan X, Shakya T, Baettig OM, Ait-Mohand-Brunet S, Berghuis AM, Wright GD, and Auclair K

Subjects
Aminoglycosides chemistry, Enterococcus faecium drug effects, Enterococcus faecium growth & development, Enzyme Inhibitors chemistry, Kanamycin pharmacology, Microbial Sensitivity Tests, Molecular Conformation, Stereoisomerism, Structure-Activity Relationship, Acetyltransferases antagonists & inhibitors, Aminoglycosides chemical synthesis, Aminoglycosides pharmacology, Coenzyme A chemistry, Enzyme Inhibitors chemical synthesis, Enzyme Inhibitors pharmacology
Abstract

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.

Published
2006
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