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Synthesis and preliminary biological evaluation of the first 99m Tc(I)‐specific semi‐rigid tridentate ligand based on a click chemistry strategy
Author(s) -
Guizani Sihem,
Malek Saied Nadia,
Picard Claude,
Benoist Eric,
Saidi Mouldi
Publication year - 2014
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3182
Subject(s) - chemistry , chelation , biodistribution , bifunctional , ligand (biochemistry) , click chemistry , combinatorial chemistry , yield (engineering) , metal , triazole , stereochemistry , in vitro , organic chemistry , receptor , biochemistry , materials science , metallurgy , catalysis
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 N 2 O 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. Copyright © 2014 John Wiley & Sons, Ltd.