Radioiodination and Biological Evaluation of Novel Quinoline Derivative for Infective Inflammation Diagnosis

This work is aimed at synthesizing a radiotracer of an iodoquinoline derivative of 2,2’-[(5-chloromethyl-8-hydroxyquinolin-7-yl) methylazanediyl] diacetic acid ([ 125 I]iodoCMHQMADA) to give a labeled compound with a radiolabeling yield of 96%. The radiotracer, [ 125 I]iodoCMHQMADA, showed high stability and purity up to 8 h using thin layer chromatography and high-performance liquid chromatography techniques. Many factors were optimized to give a high radiochemical yield. The radiotracer, [ 125 I]iodoCMHQMADA, exhibited tissue uptake (target to nontarget T/NT=7.76±0.36) in Escherichia coli- induced infection in mice, which is higher than the commercially available 99m Tc-ciprofloxacin (T/NT=3.80±0.80). Furthermore, it was able to differentiate between septic and aseptic inflammation.