Probing linker design in citric acid-ciprofloxacin conjugates

Stephen J. Milner; Anna M. Snelling; Kevin G. Kerr; Ahmad Abd-El-Aziz; Gavin H. Thomas; Roderick E. Hubbard; Anne Routledge; Anne Kathrin Duhme-Klair

doi:10.1016/j.bmc.2014.04.009

Probing linker design in citric acid-ciprofloxacin conjugates

Stephen J. Milner, Anna M. Snelling, Kevin G. Kerr, Ahmad Abd-El-Aziz, Gavin H. Thomas, Roderick E. Hubbard, Anne Routledge^*, Anne Kathrin Duhme-Klair

^*Corresponding author for this work

Research output: Contribution to journal › Article › peer-review

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. © 2014 Published by Elsevier Ltd. All rights reserved.

Original language	English
Pages (from-to)	4499-4505
Number of pages	7
Journal	Bioorganic & Medicinal Chemistry
Volume	22
Issue number	16
Early online date	15 Apr 2014
DOIs	https://doi.org/10.1016/j.bmc.2014.04.009
Publication status	Published - 15 Aug 2014

Bibliographical note

Keywords

Antibiotic
Citrate
Computational modelling
Siderophore

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10.1016/j.bmc.2014.04.009

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title = "Probing linker design in citric acid-ciprofloxacin conjugates",

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. {\textcopyright} 2014 Published by Elsevier Ltd. All rights reserved.",

keywords = "Antibiotic, Citrate, Computational modelling, Siderophore",

author = "Milner, {Stephen J.} and Snelling, {Anna M.} and Kerr, {Kevin G.} and Ahmad Abd-El-Aziz and Thomas, {Gavin H.} and Hubbard, {Roderick E.} and Anne Routledge and Duhme-Klair, {Anne Kathrin}",

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AU - Milner, Stephen J.

AU - Snelling, Anna M.

AU - Kerr, Kevin G.

AU - Abd-El-Aziz, Ahmad

AU - Thomas, Gavin H.

AU - Hubbard, Roderick E.

AU - Routledge, Anne

AU - Duhme-Klair, Anne Kathrin

PY - 2014/8/15

Y1 - 2014/8/15

N2 - 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. © 2014 Published by Elsevier Ltd. All rights reserved.

AB - 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. © 2014 Published by Elsevier Ltd. All rights reserved.

KW - Antibiotic

KW - Citrate

KW - Computational modelling

KW - Siderophore

UR - http://www.scopus.com/inward/record.url?scp=84906220907&partnerID=8YFLogxK

U2 - 10.1016/j.bmc.2014.04.009

DO - 10.1016/j.bmc.2014.04.009

M3 - Article

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SN - 0968-0896

VL - 22

SP - 4499

EP - 4505

JO - Bioorganic & Medicinal Chemistry

JF - Bioorganic & Medicinal Chemistry

IS - 16

ER -

Probing linker design in citric acid-ciprofloxacin conjugates

Abstract

Bibliographical note

Keywords

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Lecture title: Bacterial iron scavengers and how to exploit them, Sheffield

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Probing linker design in citric acid-ciprofloxacin conjugates

Abstract

Bibliographical note

Keywords

Access to Document

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Activities

Lecture title: Bacterial iron scavengers and how to exploit them, Sheffield

Cite this