Regio‐ and Chemoselective 6′‐N‐Derivatization of Aminoglycosides: Bisubstrate Inhibitors as Probes To Study Aminoglycoside 6′‐ N ‐Acetyltransferases | Zendy

Gao Feng | Zendy; Yan Xuxu | Zendy; Baettig Oliver M. | Zendy; Berghuis Albert M. | Zendy; Auclair Karine | Zendy

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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 international edition

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 5.831

H-Index - 550

eISSN - 1521-3773

pISSN - 1433-7851

DOI - 10.1002/anie.200501399

Subject(s) - acetyltransferases , aminoglycoside , acetyltransferase , chemistry , regioselectivity , derivatization , enzyme , combinatorial chemistry , acetylation , antibiotics , biochemistry , stereochemistry , chromatography , mass spectrometry , catalysis , gene

Complex nanomolar inhibitors in one pot : Aminoglycoside–coenzyme A derivatives were prepared through an efficient regioselective 6′‐N modification of aminoglycosides (see scheme). These bisubstrates show tight‐binding competitive inhibition of aminoglycoside 6′‐ N ‐acetyltransferase, an enzyme involved in antibiotic resistance.

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