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Pharmaceuticals 2010, 3(3), 679-701; doi:10.3390/ph3030679
Article

2-Deoxystreptamine Conjugates by Truncation–Derivatization of Neomycin

1, 2, 2, 2, 1 and 1,*
1 Radboud University Nijmegen, IMM Organic Chemistry, Heyendaalseweg 135, 6525 AJ, Nijmegen, the Netherlands 2 Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, 2300 RA, Leiden, the Netherlands
* Author to whom correspondence should be addressed.
Received: 18 December 2009 / Revised: 8 March 2010 / Accepted: 10 March 2010 / Published: 15 March 2010
(This article belongs to the Special Issue Antibiotics)
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Abstract

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.
Keywords: aminoglycosides; morpholine; aminopyridine; aminoquinoline; hemocyanin; biosensor; fluorescence aminoglycosides; morpholine; aminopyridine; aminoquinoline; hemocyanin; biosensor; fluorescence
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Aslam, M.W.; Tabares, L.C.; Andreoni, A.; Canters, G.W.; Rutjes, F.P.; Van Delft, F.L. 2-Deoxystreptamine Conjugates by Truncation–Derivatization of Neomycin. Pharmaceuticals 2010, 3, 679-701.

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