Glycodiversification for the Optimization of the Kanamycin Class Aminoglycosides
Journal of Medicinal Chemistry2005Vol. 48(20), pp. 6271–6285
Citations Over TimeTop 20% of 2005 papers
Jinhua Wang, Jie Li, Hsiao‐Nung Chen, Hui‐Wen Chang, Christabel Tomla Tanifum, Hsiu-Hsiang Liu, Przemyslaw G. Czyryca, Cheng‐Wei Tom Chang
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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