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

Bioorg Med Chem Lett. 2008 Oct 1;18(19):5168-70. doi: 10.1016/j.bmcl.2008.08.109. Epub 2008 Sep 3.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

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

Substances

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