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

  作者 Zhang, JB; Guo, HX; Zhang, SJ; Lin, Y; Wang, XB  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2008年18-19;  页码  5168-5170  
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[摘要]The ciprofloxacin dithiocarbamate (CPFXDTC) was synthesized and radiolabeled with [(TcN)-Tc-99m](2+) intermediate to form the (TcN)-Tc-99m-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 (TcN)-Tc-99m-CPFXDTC had a better binding affinity as compared with Tc-99m-ciprofloxacin. Biodistribution results in induced infection mice showed (TcN)-Tc-99m-CPFXDTC had higher uptake at the sites of infection and better abscess/blood ratio than that of Tc-99m-ciprofloxacin, suggesting (TcN)-Tc-99m-CPFXDTC would be a novel potential infection imaging agent. (C) 2008 Elsevier Ltd. All rights reserved.

 
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