Novel lipophilic amidate oxorhenium and oxotechnetium complexes as potential brain agents: Synthesis, characterization and biological evaluation

 
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2001 (EN)
Novel lipophilic amidate oxorhenium and oxotechnetium complexes as potential brain agents: Synthesis, characterization and biological evaluation (EN)

Papadopoulos, M. (EN)

Πανεπιστήμιο Ιωαννίνων. Σχολή Θετικών Επιστημών. Τμήμα Χημείας (EL)
Papadopoulos, M. (EN)

Novel oxorhenium and oxotechnetium complexes based on the tetradentate 1-(2-hydroxybenzamido)-2-(pyridinecarboxamido)benzene, H3L, ligand have been synthesized and characterized herein. Thus, by reacting equimolar quantities of the triply deprotonated ligand L3- With the suitable MO3+ precursor, the following neutral MOL complexes could be easily produced following similar synthetic routes: M=Re (1), M=(TC)-T-99g (2) and M=Tc-99m (3). Complexes 1 and 2, prepared in macroscopic amounts, were chemically characterized and their structure determined by single-crystal X-ray analysis. They are isostructural metal chelates, adopting a distorted square pyramidal geometry around the metal. The N3O donor atom set of the tetradentate ligand defines the basal plane and the oxygen atom of the M=O core occupies the apex of the pyramid. Complex 3 forms quantitatively at tracer level by mixing the H3L ligand with (NaTcO4)-Tc-99m generator eluate in aqueous alkaline media and using tin chloride as reductant in the presence of citrate. Its structure was established by chromatographic comparison with prototypic complexes 1 and 2 using high-performance liquid chromatographic techniques. When challenged with excess glutathione in vitro, complex 3 is rapidly converted to hydrophilic unidentified metal species. Tissue distribution data after administration of complex 3 in vivo revealed a significant uptake and retention of this compound in brain tissue. (EN)

rhenium (EN)

Πανεπιστήμιο Ιωαννίνων (EL)
University of Ioannina (EN)

Journal of Biological Inorganic Chemistry (EN)

English

2001

<Go to ISI>://000167176900007

Springer Verlag (Germany) (EN)



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