2-Deoxystreptamine Conjugates by Truncation–Derivatization of Neomycin

Autor: Floris L. van Delft, Floris P.J.T. Rutjes, Gerard W. Canters, Alessio Andreoni, Leandro C. Tabares, M. Waqar Aslam
Jazyk: angličtina
Rok vydání: 2010
Předmět:
Zdroj: Pharmaceuticals, Vol 3, Iss 3, Pp 679-701 (2010)
Druh dokumentu: article
ISSN: 1424-8247
DOI: 10.3390/ph3030679
Popis: 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.
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