title: Synthesis and preliminary biological evaluation of the first (99m)Tc(I)-specific semi-rigid tridentate ligand based on a click chemistry strategy.
abstract: 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.
authors.affiliation: Radiopharmaceutical Unit, Centre National des Sciences et Technologies Nucléaires, Sidi Thabet, 2020, Tunisia.
authors.forename: Sihem
authors.initials: S
authors.lastname: Guizani
authors.forename: Nadia
authors.initials: N
authors.lastname: Malek Saied
authors.forename: Claude
authors.initials: C
authors.lastname: Picard
authors.forename: Eric
authors.initials: E
authors.lastname: Benoist
authors.forename: Mouldi
authors.initials: M
authors.lastname: Saidi
mesh_terms: D000627:Aminophenols / Q000737:chemistry; D000818:Animals; D057930:Click Chemistry; D004355:Drug Stability; D008024:Ligands; D008297:Male; D051379:Mice; D015609:Organotechnetium Compounds / Q000138:chemical synthesis* / Q000737:chemistry* / Q000493:pharmacokinetics; D011854:Radiochemistry; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry* / Q000493:pharmacokinetics; D014230:Triazoles / Q000737:chemistry
chemical_list: D000627:Aminophenols; D008024:Ligands; D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; D014230:Triazoles; C027667:2-aminophenol
keywords: bifunctional chelating agent; click chemistry; technetium-99m; tissue distribution