Synthesis and biodistribution of a novel (99m)TcN complex of ciprofloxacin dithiocarbamate as a potential agent for infection imaging.

Abstract

The ciprofloxacin dithiocarbamate (CPFXDTC) was synthesized and radiolabeled with [(99m)TcN](2+) intermediate to form the (99m)TcN-CPFXDTC complex in high yield (>95%). No decomposition of the complex at room temperature was observed over a period of 6 h. Its partition coefficient indicated that it was a good lipophilic complex. The bacterial binding assay studies showed (99m)TcN-CPFXDTC had a better binding affinity as compared with (99m)Tc-ciprofloxacin. Biodistribution results in induced infection mice showed (99m)TcN-CPFXDTC had higher uptake at the sites of infection and better abscess/blood ratio than that of (99m)Tc-ciprofloxacin, suggesting (99m)TcN-CPFXDTC would be a novel potential infection imaging agent.

• Authors: Junbo Zhang, Haixun Guo, Shijian Zhang, Yan Lin, Xuebin Wang
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 18 Issue 19 Pg. 5168-70 (Oct 01 2008) ISSN: 1464-3405 [Electronic] England
• PMID: 18790638 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• 99mTc-CPFXDTC
• Organotechnetium Compounds
• Radiopharmaceuticals
• Thiocarbamates
• ciprofloxacin dithiocarbamate
• Ciprofloxacin

Topics

• Animals
• Ciprofloxacin (analogs & derivatives, blood, chemical synthesis, pharmacokinetics)
• Diagnostic Imaging
• Male
• Mice
• Molecular Structure
• Organotechnetium Compounds (blood, chemical synthesis, pharmacokinetics)
• Radiopharmaceuticals
• Thiocarbamates (blood, chemical synthesis, pharmacokinetics)
• Tissue Distribution
• Whole-Body Counting