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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Detalles Bibliográficos
Autores principales: Aslam, M. Waqar, Tabares, Leandro C., Andreoni, Alessio, Canters, Gerard W., Rutjes, Floris P.J.T., van Delft, Floris L.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Molecular Diversity Preservation International 2010
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4033975/
https://www.ncbi.nlm.nih.gov/pubmed/27713274
http://dx.doi.org/10.3390/ph3030679
Descripción
Sumario: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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