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A Click procedure with heterogeneous copper to tether technetium-99m chelating agents and rhenium complexes. Evaluation of the chelating properties and biodistribution of the new radiolabelled glucose conjugates
- Benoist, Eric, Coulais, Yvon, Almant, Mehdi, Kovensky, José, Moreau, Vincent, Lesur, David, Artigau, Marine, Picard, Claude, Galaup, Chantal, Gouin, Sébastien G.
- Carbohydrate research 2011 v.346 no.1 pp. 26-34
- catalysts, chelating agents, copper, glucose, glycoconjugates, pharmacokinetics, radiolabeling, rhenium, spleen, stomach, technetium
- An efficient protocol was developed to tether chelating agents and rhenium complexes onto a glucoside scaffold with a heterogeneous copper catalyst via click chemistry. The supported catalyst avoids the formation of unwanted copper complexes during the cyclisation step. The possibility to graft a pre-chelated M(CO)₃ core by click chemistry onto a biomolecule was highlighted for the first time. ⁹⁹ᵐTc(CO)₃-glucoconjugates displayed excellent in vitro stability, a fast in vivo blood clearance and a low specific organ uptake or long-term retention in spleen and stomach.