title: 2-Deoxystreptamine Conjugates by Truncation-Derivatization of Neomycin.
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-resistantE. coli.
authors.affiliation: Radboud University Nijmegen, IMM Organic Chemistry, Heyendaalseweg 135, 6525 AJ, Nijmegen, the Netherlands.
authors.forename: M Waqar
authors.initials: MW
authors.lastname: Aslam
authors.affiliation: Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, 2300 RA, Leiden, the Netherlands.
authors.forename: Leandro C
authors.initials: LC
authors.lastname: Tabares
authors.affiliation: Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, 2300 RA, Leiden, the Netherlands.
authors.forename: Alessio
authors.initials: A
authors.lastname: Andreoni
authors.affiliation: Leiden Institute of Chemistry, Leiden University, Einsteinweg 55, 2300 RA, Leiden, the Netherlands.
authors.forename: Gerard W
authors.initials: GW
authors.lastname: Canters
authors.affiliation: Radboud University Nijmegen, IMM Organic Chemistry, Heyendaalseweg 135, 6525 AJ, Nijmegen, the Netherlands.
authors.forename: Floris P J T
authors.initials: FP
authors.lastname: Rutjes
authors.affiliation: Radboud University Nijmegen, IMM Organic Chemistry, Heyendaalseweg 135, 6525 AJ, Nijmegen, the Netherlands. f.vandelft@science.ru.nl.
authors.forename: Floris L
authors.initials: FL
authors.lastname: Van Delft
keywords: aminoglycosides; aminopyridine; aminoquinoline; biosensor; fluorescence; hemocyanin; morpholine