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  • Title: Glycodiversification for the optimization of the kanamycin class aminoglycosides.
    Author: Wang J, Li J, Chen HN, Chang H, Tanifum CT, Liu HH, Czyryca PG, Chang CW.
    Journal: J Med Chem; 2005 Oct 06; 48(20):6271-85. PubMed ID: 16190754.
    Abstract:
    In an effort to optimize the antibacterial activity of kanamycin class aminoglycoside antibiotics, we have accomplished the synthesis and antibacterial assay of new kanamycin B analogues. A rationale-based glycodiversification strategy was employed. The activity of the lead is comparable to that of commercially available kanamycin. These new members, however, were found to be inactive against aminoglycoside resistant bacteria. Molecular modeling was used to provide the explanation. Thus, a new strategy for structural modifications of kanamycin class aminoglycosides is suggested.
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