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Regio‐ and Chemoselective 6′‐N‐Derivatization of Aminoglycosides: Bisubstrate Inhibitors as Probes To Study Aminoglycoside 6′‐ N ‐Acetyltransferases
Author(s) -
Gao Feng,
Yan Xuxu,
Baettig Oliver M.,
Berghuis Albert M.,
Auclair Karine
Publication year - 2005
Publication title -
angewandte chemie
Language(s) - German
Resource type - Journals
eISSN - 1521-3757
pISSN - 0044-8249
DOI - 10.1002/ange.200501399
Subject(s) - acetyltransferases , chemistry , derivatization , acetyltransferase , stereochemistry , acetylation , biochemistry , organic chemistry , high performance liquid chromatography , gene
Einfach zu komplexen nanomolaren Inhibitoren : Aminoglycosid‐Coenzym‐A‐Derivate wurden durch eine effiziente regioselektive 6′‐N‐Modifizierung von Aminoglycosiden hergestellt (siehe Schema). Diese Bisubstrate sind fest bindende kompetitive Inhibitoren der Aminoglycosid‐6′‐ N ‐Acetyltransferase, eines an der Antibiotikaresistenz beteiligten Enzyms.

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