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  • Title: Evaluation of amphiphilic aminoglycoside-peptide triazole conjugates as antibacterial agents.
    Author: Bera S, Zhanel GG, Schweizer F.
    Journal: Bioorg Med Chem Lett; 2010 May 15; 20(10):3031-5. PubMed ID: 20413307.
    Abstract:
    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.
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