期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 10, 页码 3031-3035出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.03.116
关键词
Aminoglycosides; Peptides; Cationic amphiphiles; Dipolar cycloaddition; MRSA
资金
- Canadian Institutes of Health Research (CIHR)
- Manitoba Health Research Council (MHRC)
- Natural Sciences and Engineering Research Council of Canada (NSERC)
- Canadian Foundation for Innovation (CFI)
The solid-and solution-phase synthesis of amphiphilic aminoglycoside-peptide triazole conjugates (APTCs) accessed by copper(I)-catalyzed 1,3-dipolar cycloaddition reaction between a hydrophobic and ultrashort peptide-based alkyne and a neomycin B-or kanamycin A-derived azide is presented. Antibacterial evaluation demonstrates that the antibacterial potency is affected by the nature of the peptide component. Several APTCs exhibit superior activity against neomycin B-and kanamycin A-resistant strains when compared to their parent aminoglycoside while displaying reduced activity against neomycin B-and kanamycin A-susceptible strains. (C) 2010 Elsevier Ltd. All rights reserved.
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