期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 15, 期 8, 页码 2944-2951出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2007.02.009
关键词
antibiotic; A-site; neamine; regioselective; resistance; aminoglycoside; acetyltransferase; antibacterial; RNA
资金
- Canadian Institutes of Health Research [85062] Funding Source: Medline
Aminoglycoside antibiotics act by binding to 16S rRNA. Resistance to these antibiotics occurs via drug modifications by enzymes such as aminoglycoside 6'-N-acetyltransferases (AAC(6')s). We report here the regioselective and efficient synthesis of N-6'-acylated aminoglycosides and their use as probes to study AAC(6')-Ii and aminoglycoside-RNA complexes. Our results emphasize the central role of N-6' nucleophilicity for transformation by AAC(6')-Ii and the importance of hydrogen bonding between 6'-NH2 and 16S rRNA for antibacterial activity. (c) 2007 Elsevier Ltd. All rights reserved.
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