PIDAZTA: Structurally Constrained Chelators for Efficient Formation of Stable Gallium-68 Complexes at Physiological pH.

Author(s) Giovenzana, G.Battista; Farkas, E.; Vágner, A.; Negri, R.; Lattuada, L.; Tóth, I.; Colombo, V.; Esteban-Gómez, D.; Platas-Iglesias, C.; Notni, J.; Baranyai, Z.
Journal Chemistry
Date Published 2019 May 31

Two structurally constrained chelators based on a fused bicyclic scaffold, [(4R*,10aS*)-PIDAZTA (L1) and (4R*,10aR*)-PIDAZTA (L2)], were designed for the preparation of GaIII-based radiopharmaceuticals. The stereochemistry of the ligand scaffold has a deep impact on the properties of the complexes, with unexpected [Ga(L2)OH] species being superior in terms of both thermodynamic stability and inertness. This peculiar behavior was rationalized on the basis of molecular modeling and appears to be related to a better fit in size of GaIII into the cavity of L2. Fast and efficient formation of the GaIII-chelates at room temperature was observed at pH values between 7 and 8, which enables 68Ga radiolabeling under truly physiological conditions (pH 7.4).

DOI 10.1002/chem.201901512
ISSN 1521-3765
Citation Chemistry. 2019.

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