99mTc(CO)3-tosufloxacin dithiocarbamate complexation and radiobiological evaluation in male Wister rat model

Dithiocarbamate complexes as radiopharmaceuticals for medical imaging

“…Dithiocarbamate derivatives of a number of antibiotic molecules based on the fluoroquinolene group have been synthesised by addition of CS 2 to a native amine group, and their [ 99m TcN(DTC) 2 ] complexes have been evaluated as infection imaging agents. These include [ 99m TcN(Ciprofloxacin-DTC) 2 ] (4) [12] and analogues based on Norfloxacin [48], Garenoxacin [49], Trovafloxacin [50], Moxifloxacin [51], Tosufloxacin [52], Sitafloxacin [53] and Gatifloxacin [54]. A [ 99m TcN(DTC) 2 ] complex based on a benzamide structure (5) was synthesised and evaluated for diagnosis of malignant melanoma [22], however, tumour/organ ratios in mice were lower than for the more established [ 123 I-BZA].…”

“…Alternatively, a monodentate phosphine ligand could be used as the bifunctional linker (17) [74]. [ 99m Tc(CO) 3 ] + has also been used to radiolabel a range of dithiocarbamate compounds including brain perfusion agents [75], 5-HT 1A receptor imaging agents [26] and dithiocarbamate derivatives of Ciprofloxacin [13], Tosufloxacin [52] and Sitafloxacin [76] for infection imaging. Whilst it is expected that the dithiocarbamate ligand coordinates to the technetium in bidentate mode, the identity of the ligand in the sixth coordination site, and the overall structure of the complex, remains unknown.…”