Cargando…

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...

Descripción completa

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:
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
_version_ 1782317908110606336
author Aslam, M. Waqar
Tabares, Leandro C.
Andreoni, Alessio
Canters, Gerard W.
Rutjes, Floris P.J.T.
van Delft, Floris L.
author_facet Aslam, M. Waqar
Tabares, Leandro C.
Andreoni, Alessio
Canters, Gerard W.
Rutjes, Floris P.J.T.
van Delft, Floris L.
author_sort Aslam, M. Waqar
collection PubMed
description 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.
format Online
Article
Text
id pubmed-4033975
institution National Center for Biotechnology Information
language English
publishDate 2010
publisher Molecular Diversity Preservation International
record_format MEDLINE/PubMed
spelling pubmed-40339752014-05-27 2-Deoxystreptamine Conjugates by Truncation–Derivatization of Neomycin Aslam, M. Waqar Tabares, Leandro C. Andreoni, Alessio Canters, Gerard W. Rutjes, Floris P.J.T. van Delft, Floris L. Pharmaceuticals (Basel) Article 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. Molecular Diversity Preservation International 2010-03-15 /pmc/articles/PMC4033975/ /pubmed/27713274 http://dx.doi.org/10.3390/ph3030679 Text en © 2010 by the authors; licensee Molecular Diversity Preservation International, Basel, Switzerland. http://creativecommons.org/licenses/by/3.0/ This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Aslam, M. Waqar
Tabares, Leandro C.
Andreoni, Alessio
Canters, Gerard W.
Rutjes, Floris P.J.T.
van Delft, Floris L.
2-Deoxystreptamine Conjugates by Truncation–Derivatization of Neomycin
title 2-Deoxystreptamine Conjugates by Truncation–Derivatization of Neomycin
title_full 2-Deoxystreptamine Conjugates by Truncation–Derivatization of Neomycin
title_fullStr 2-Deoxystreptamine Conjugates by Truncation–Derivatization of Neomycin
title_full_unstemmed 2-Deoxystreptamine Conjugates by Truncation–Derivatization of Neomycin
title_short 2-Deoxystreptamine Conjugates by Truncation–Derivatization of Neomycin
title_sort 2-deoxystreptamine conjugates by truncation–derivatization of neomycin
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4033975/
https://www.ncbi.nlm.nih.gov/pubmed/27713274
http://dx.doi.org/10.3390/ph3030679
work_keys_str_mv AT aslammwaqar 2deoxystreptamineconjugatesbytruncationderivatizationofneomycin
AT tabaresleandroc 2deoxystreptamineconjugatesbytruncationderivatizationofneomycin
AT andreonialessio 2deoxystreptamineconjugatesbytruncationderivatizationofneomycin
AT cantersgerardw 2deoxystreptamineconjugatesbytruncationderivatizationofneomycin
AT rutjesflorispjt 2deoxystreptamineconjugatesbytruncationderivatizationofneomycin
AT vandelftflorisl 2deoxystreptamineconjugatesbytruncationderivatizationofneomycin