Synthesis and preliminary biological evaluation of the first (99m)Tc(I)-specific semi-rigid tridentate ligand based on a click chemistry strategy

A novel bifunctional chelating agent based on a click chemistry strategy has been synthesized and characterized on the basis of spectroscopic techniques. The metal chelating part of this new class of tridentate N2O ligand combined a triazole unit and an aromatic ring. This latter semi-rigid framewor...

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Bibliographic Details
Published in:Journal of labelled compounds & radiopharmaceuticals 2014-03, Vol.57 (3), p.158-163
Main Authors: Guizani, Sihem, Malek Saied, Nadia, Picard, Claude, Benoist, Eric, Saidi, Mouldi
Format: Article
Language:English
Subjects:
Aminophenols - chemistry
Animals
Click Chemistry
Drug Stability
Ligands
Male
Mice
Organotechnetium Compounds - chemical synthesis
Organotechnetium Compounds - chemistry
Organotechnetium Compounds - pharmacokinetics
Radiochemistry
Radiopharmaceuticals - chemical synthesis
Radiopharmaceuticals - chemistry
Radiopharmaceuticals - pharmacokinetics
Triazoles - chemistry
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Summary:A novel bifunctional chelating agent based on a click chemistry strategy has been synthesized and characterized on the basis of spectroscopic techniques. The metal chelating part of this new class of tridentate N2O ligand combined a triazole unit and an aromatic ring. This latter semi-rigid framework induced a pre-organization of the chelating cavity, improving the stability of the corresponding metallic complexes (M = (99m) Tc, Re). Thus, the (99m) Tc(CO)3 complex, obtained with good yield and excellent radiochemical purity (>90%), exhibited a high in vitro serum stability. Tissue biodistribution in normal mice showed a rapid clearance, no long-term retention in organs and no in vivo reoxidation of technetium-99m, making this compound a promising (99m)Tc-chelating system.
ISSN:1099-1344
DOI:10.1002/jlcr.3182