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Accelerating water exchange for GdIII chelates by steric compression around the water binding site
Robert Ruloff1, Eva Tóth, Rosario Scopelliti
1Ecole Polytechnique Fédérale de Lausanne, ICMB, BCH, Lausanne, Switzerland.
Abstract:
The water exchange process was accelerated for nine-coordinate, monohydrated macrocyclic GdIII complexes by inducing steric compression around the water binding site; the increased steric crowding was achieved by replacing an ethylene bridge of DOTA4- by a propylene bridge; in addition to the optimal water exchange rate, the stability of [Gd(TRITA)(H2O)]- is sufficiently high to ensure safe medical use which makes it a potential synthon for the development of high relaxivity, macromolecular MRI contrast agents.