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 iscomparable to that of commercially available kanamycin. These new members, however, werefound to be inactive against aminoglycoside resistant bacteria. Molecular modeling was usedto provide the explanation. Thus, a new strategy for structural modifications of kanamycinclass aminoglycosides is suggested.
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