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Benzimidazole derivatives as NSO ligands for the fac-[M(CO)3] (M = Re, Tc)
Authors:T Tsotakos  G Patsis  N Nikoli?  D Djoki?  A Terzis  M Pelecanou  I Pirmettis
Institution:a Institute of Radioisotopes - Radiodiagnostic Products, National Center for Scientific Research “Demokritos”, 15310 Ag. Paraskevi, Athens, Greece
b Institute of Biology, National Center for Scientific Research “Demokritos”, 15310 Ag. Paraskevi, Athens, Greece
c University of Belgrade, Vinca Institute of Nuclear Sciences, Laboratory for Radioisotopes, P.O.B. 522, 11001 Belgrade, Serbia
d Institute of Materials Science, National Center for Scientific Research “Demokritos”, 15310 Ag. Paraskevi, Athens, Greece
e Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotle University of Thessaloniki, Thessaloniki 54124, Greece
Abstract:Two rhenium(I) tricarbonyl complexes with the tridentate monoanionic NSO ligands, 4-(benzimidazol-2-yl)-3-thiabutanoic acid (complex 3) and 1-(11-carboxyundecanyl)-4-(benzimidazol-2-yl)]-3-thiabutanoic acid (complex 4) were synthesized and characterized by spectroscopic methods and elemental analysis. X-ray crystallographic analysis of complex 3 revealed a distorted octahedral geometry around rhenium defined by the three facially bound CO groups and the NSO donor atom set of the tridentate ligand. The analogous technetium-99m complexes (complexes 5 and 6) were also prepared quantitatively by reaction of the NSO ligands with the fac-99mTc(H2O)3(CO)3]+ synthon and their identity was established by chromatographic comparison to their rhenium congeners. Biodistribution in mice of complex 6 bearing the fatty acid chain showed significant heart uptake (6.26 ± 0.79% ID/g p.i.) at 1 min accompanied, however, with a heart:blood ratio below 1.
Keywords:Technetium-99m  Rhenium  Tricarbonyl  Fatty acid
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