title: 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.
abstract: 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. (99m)Tc(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.
authors.affiliation: Laboratoire de Synthèse et Physico-Chimie de Molécules d'Intérêt Biologique, SPCMIB, UMR 5068, 118, route de Narbonne, F-31062 Toulouse cedex 9, France. benoist@chimie.ups-tlse.fr
authors.forename: Eric
authors.initials: E
authors.lastname: Benoist
authors.forename: Yvon
authors.initials: Y
authors.lastname: Coulais
authors.forename: Mehdi
authors.initials: M
authors.lastname: Almant
authors.forename: José
authors.initials: J
authors.lastname: Kovensky
authors.forename: Vincent
authors.initials: V
authors.lastname: Moreau
authors.forename: David
authors.initials: D
authors.lastname: Lesur
authors.forename: Marine
authors.initials: M
authors.lastname: Artigau
authors.forename: Claude
authors.initials: C
authors.lastname: Picard
authors.forename: Chantal
authors.initials: C
authors.lastname: Galaup
authors.forename: Sébastien G
authors.initials: SG
authors.lastname: Gouin
mesh_terms: D002614:Chelating Agents / Q000737:chemistry*; D057930:Click Chemistry / Q000379:methods*; D003300:Copper / Q000737:chemistry*; D005947:Glucose / Q000737:chemistry*; D006001:Glycoconjugates / Q000138:chemical synthesis* / Q000737:chemistry; D015394:Molecular Structure; D015609:Organotechnetium Compounds / Q000138:chemical synthesis* / Q000737:chemistry; D012211:Rhenium / Q000737:chemistry*; D013667:Technetium / Q000737:chemistry*
chemical_list: D002614:Chelating Agents; D006001:Glycoconjugates; D015609:Organotechnetium Compounds; D012211:Rhenium; D013667:Technetium; D003300:Copper; D005947:Glucose