Jump to main content
Jump to site search

Issue 5, 2009
Previous Article Next Article

Synthesis and evaluation of Ciprofloxacin derivatives as diagnostic tools for bacterial infection by Staphylococcus aureus

Author affiliations

Abstract

Development of target-specific diagnostic radiopharmaceuticals has always been a challenging task. For this purpose, design and development of the imaging-friendly variant of a potent antibiotic could aid in treatment planning and follow-up of patients with hard-to-diagnose bacterial infections. Fluoroquinolone analogues were synthesized taking the lead from Ciprofloxacin (the broad spectrum antibiotic) molecule. The idea of modifying fluoroquinolones, and subsequently labeling them, was to preserve their capacity to bind bacteria and thereby enable the compound to specifically target those microorganisms. Three compounds were thus synthesized as derivatives of Ciprofloxacin. The fluoroquinolone analogues were labeled with 99mTc by using 99mTc pertechnetate with high labeling efficiency for all the formulations. The complexes formed by chelation of 99mTc with our synthesized fluoroquinolone analogues showed good in vitro serum stability. The blood clearance study performed in New Zealand White rabbits exhibited a curve indicating the initial fast phase in which radiocomplexed drugs cleared from blood very quickly followed by a slow phase. The in vivo evaluation showed that fluoroquinolone-based radiopharmaceuticals bind to the bacteria present at the site of infection, which results in the retention of the agent at sites of active bacterial infection. The biodistribution data and the scintigrams demonstrated that Staphylococcus aureus bacteria in animal infection models took up the radiopharmaceutical formulations, confirming our hypothesis that 99mTc fluoroquinolone derivatives might be useful as diagnostic agents for targeted delivery in bacterial infections.

Graphical abstract: Synthesis and evaluation of Ciprofloxacin derivatives as diagnostic tools for bacterial infection by Staphylococcus aureus

Back to tab navigation

Supplementary files

Article information


Submitted
28 Apr 2009
Accepted
30 Jun 2009
First published
05 Aug 2009

Metallomics, 2009,1, 409-417
Article type
Paper

Synthesis and evaluation of Ciprofloxacin derivatives as diagnostic tools for bacterial infection by Staphylococcus aureus

S. Dahiya, K. Chuttani, R. K. Khar, D. Saluja, A. K. Mishra and M. Chopra, Metallomics, 2009, 1, 409
DOI: 10.1039/B908474F

Social activity

Search articles by author

Spotlight

Advertisements