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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,*
Received: 18 December 2009; in revised form: 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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MDPI and ACS Style

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.

AMA Style

Aslam MW, Tabares LC, Andreoni A, Canters GW, Rutjes FP, Van Delft FL. 2-Deoxystreptamine Conjugates by Truncation–Derivatization of Neomycin. Pharmaceuticals. 2010; 3(3):679-701.

Chicago/Turabian Style

Aslam, M. Waqar; Tabares, Leandro C.; Andreoni, Alessio; Canters, Gerard W.; Rutjes, Floris P.J.T.; Van Delft, Floris L. 2010. "2-Deoxystreptamine Conjugates by Truncation–Derivatization of Neomycin." Pharmaceuticals 3, no. 3: 679-701.


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