Probing bacterial uptake of glycosylated ciprofloxacin conjugates

Stephen J Milner, Christopher T Carrick, Kevin G Kerr, Anna M Snelling, Gavin H Thomas, Anne-Kathrin Duhme-Klair, Anne Routledge

Research output: Contribution to journalArticlepeer-review


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.
Original languageEnglish
Pages (from-to)466-471
Number of pages6
Issue number3
Early online date21 Jan 2014
Publication statusPublished - 10 Feb 2014

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Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

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