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.

• Authors: 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
• Journal: Bioorganic & medicinal chemistry (Bioorg Med Chem) Vol. 22 Issue 16 Pg. 4499-505 (Aug 15 2014) ISSN: 1464-3391 [Electronic] England
• PMID: 24794750 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: Copyright © 2014 Elsevier Ltd. All rights reserved.

Chemical References

• Anti-Bacterial Agents
• Topoisomerase II Inhibitors
• Citric Acid
• Ciprofloxacin
• DNA Gyrase

Topics

• Anti-Bacterial Agents (chemical synthesis, chemistry, pharmacology)
• Bacteria (drug effects)
• Ciprofloxacin (chemistry, pharmacology)
• Citric Acid (chemistry, pharmacology)
• DNA Gyrase (metabolism)
• Dose-Response Relationship, Drug
• Drug Design
• Humans
• Microbial Sensitivity Tests
• Models, Molecular
• Molecular Structure
• Structure-Activity Relationship
• Topoisomerase II Inhibitors (chemical synthesis, chemistry, pharmacology)