2-Deoxystreptamine Conjugates by Truncation-Derivatization of Neomycin

A small library of truncated neomycin-conjugates is prepared by consecutive removal of 2,6-diaminoglucose rings, oxidation-reductive amination of ribose, oxidation-conjugation of aminopyridine/aminoquinoline and finally dimerization. The dimeric conjugates were evaluated for antibacterial activity w...

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Main Authors: Floris L. van Delft (Author), Floris P.J.T. Rutjes (Author), Gerard W. Canters (Author), Alessio Andreoni (Author), Leandro C. Tabares (Author), M. Waqar Aslam (Author)
Format: Book
Published: MDPI AG, 2010-03-01T00:00:00Z.
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Summary:A small library of truncated neomycin-conjugates is prepared by consecutive removal of 2,6-diaminoglucose rings, oxidation-reductive amination of ribose, oxidation-conjugation of aminopyridine/aminoquinoline and finally dimerization. The dimeric conjugates were evaluated for antibacterial activity with a unique hemocyanin-based biosensor. Based on the outcome of these results, a second-generation set of monomeric conjugates was prepared and found to display significant antibacterial activity, in particular with respect to kanamycin-resistant E. coli.
Item Description:10.3390/ph3030679
1424-8247