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Bioorg Med Chem. 2014 Aug 15;22(16):4499-505. doi: 10.1016/j.bmc.2014.04.009. Epub 2014 Apr 15.

Probing linker design in citric acid-ciprofloxacin conjugates.

Author information

1
Department of Chemistry, University of York, Heslington, York YO10 5DD, UK.
2
Bradford Infection Group, University of Bradford, Bradford BD7 1DP, UK.
3
Department of Microbiology, Fewston Wing, Harrogate District Hospital, Harrogate HG2 7SX, UK; Department of Biology (Area 10), University of York, Heslington, York YO10 5DD, UK; Hull York Medical School, Heslington, York YO10 5DD, UK.
4
Department of Chemistry, University of York, Heslington, York YO10 5DD, UK; Department of Biology (Area 10), University of York, Heslington, York YO10 5DD, UK.
5
Department of Biology (Area 10), University of York, Heslington, York YO10 5DD, UK.
6
Department of Chemistry, University of York, Heslington, York YO10 5DD, UK; Vernalis (R&D) Ltd, Granta Park, Cambridge CB21 6GB, UK.
7
Department of Chemistry, University of York, Heslington, York YO10 5DD, UK. Electronic address: anne.routledge@york.ac.uk.
8
Department of Chemistry, University of York, Heslington, York YO10 5DD, UK. Electronic address: anne.duhme-klair@york.ac.uk.

Abstract

A series of structurally related citric acid-ciprofloxacin conjugates was synthesised to investigate the influence of the linker between citric acid and ciprofloxacin on antibacterial activities. Minimum inhibitory concentrations (MICs) were determined against a panel of reference strains and clinical isolates of bacteria associated with infection in humans and correlated with the DNA gyrase inhibitory activity. The observed trend was rationalised by computational modelling.

KEYWORDS:

Antibiotic; Citrate; Computational modelling; Siderophore

PMID:
24794750
DOI:
10.1016/j.bmc.2014.04.009
[Indexed for MEDLINE]

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