Publication

Probing bacterial uptake of glycosylated ciprofloxacin conjugates

Milner, S.J.
; 
Carrick, C. .
; 
Kerr, Kevin G.
; 
Snelling, Anna M.
; 
Thomas, G.H.
; 
Duhme-Klair, A-K.
; 
Routledge, A.
Publication Date
2014
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Keywords
Anti-bacterial agents, Bacterial proteins, Ciprofloxacin, DNA gyrase, Disaccharides, Disk diffusion antimicrobial tests, Glycoconjugates, Glycosylation, Gram-negative bacteria, Gram-positive bacteria, Monosaccharides, Antiobiotics, Bacteria, Carbohydrates, Ciprofloxacin, Uptake
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Life Sciences Publications
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Abstract
Mono- and disaccharide-functionalised conjugates of the fluoroquinolone antibiotic ciprofloxacin have been synthesised and used as chemical probes of the bacterial uptake of glycosylated ciprofloxacin. Their antimicrobial activities against a panel of clinically relevant bacteria were determined: the ability of these conjugates to inhibit their target DNA gyrase and to be transported into the bacteria was assessed by using in vivo and in vitro assays. The data suggest a lack of active uptake through sugar transporters and that although the addition of monosaccharides is compatible with the inhibition of DNA gyrase, the addition of a disaccharide results in a significant decrease in antimicrobial activity.
URI
http://hdl.handle.net/10454/10511
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Citation
Milner SJ, Carrick CT, Kerr KG et al (2014) Probing bacterial uptake of glycosylated ciprofloxacin conjugates. Chembiochem. 15(3): 466-471.
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https://doi.org/10.1002/cbic.201300512
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