Fast and easy access to efficient bifunctional chelators for MRI applications

Equilibrium, Kinetic and Structural Properties of Gallium(III) and Some Divalent Metal Complexes Formed with the New DATAm and DATA5m Ligands

“…[15] Its coordination properties towards a wide array of metal ions have been reported, showing its remarkable affinities to lanthanides and transition metal ions. [16][17][18][19] The ready availability of AAZTA and recent descriptions of its lipophilic derivatives for targeting high density lipoproteins (HDL), [20] cell FULL PAPER membranes, [21] the synthesis of bifunctional compounds for conjugation purposes, [22] and the fast formation of complexes prompted us to explore the possibility of employing the AAZTA platform for developing useful complexes for targeted PET applications. [23] Based on the 6-amino-1,4-diazapine (DATA) scaffold new hexadentate chelators were developed by Waldron et al that shows favourable complexation behaviour.…”

Strategies for the covalent conjugation of a bifunctional chelating agent to albumin: Synthesis and characterization of potential MRI contrast agents

“…To avoid possible weakening of the gadolinium complexation that may lead to the release of free Gd 3+ ions a number of bifunctional chelating agents (BFCA) have been developed [12,18,19]. Bifunctional ligands have been designed to bind tightly to the metal ion, while a further functionality acts as a linker to the macromolecule.…”

Preparation, crystallographic and theoretical study on a bifunctional Gd-AAZTA derivative as potential MRI contrast agent precursor

“…Additional derivatives of the parent ligand include: (i) an additional lipophilic double-chain AAZTA, successfully employed to label cells on their outer surface [17], (ii) bifunctional derivatives useful for conjugation to vectors [18,19], (iii) oligomers such as a dimer [20], where the relaxivity is more than doubled than that of the monomeric Gd-AAZTA in virtue of a significant contribution arising from the increased molecular reorientational time and from water molecules in the second coordination sphere of the Gd(III) ions, and multimers where up to 8 Gd-AAZTA units were linked to a central PAMAM dendrimeric scaffold [21].…”