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Investigation of the complexation of natZr(iv) and 89Zr(iv) by hydroxypyridinones for the development of chelators for PET imaging applications.


ABSTRACT: Three hydroxypyridinone (HOPO) positional isomers - 1,2-HOPO (L1H) and its water soluble analogue (L1'H), 3,2-HOPO (L2H) and 3,4-HOPO (L3H) have been investigated for the complexation of Zr(iv). Potentiometric and UV-Vis spectrometric studies show a higher thermodynamic stability for the formation of Zr(L1')4 in comparison with Zr(L2)4 and Zr(L3)4 as well as a higher kinetic inertness in competition studies with EDTA or Fe3+ at a radiotracer concentration with 89Zr. Besides the low pKa of L1H or L1'H (pKa = 5.01) in comparison with L2H and L3H (pKa = 8.83 and 9.55, respectively), the higher stability of Zr(L1')4 can be attributed in part to the presence of the amide group next to the chelating oxygen that induces intramolecular H-bond and amide/? interactions that were observed by X-ray crystallography and confirmed by quantum chemical calculations. The data presented here indicate that the 1,2-HOPO L1' exhibits the best characteristics for Zr(iv) complexation. However, 3,2-HOPO and 3,4-HOPO patterns, if appropriately tuned, for instance with the addition of an amide group as in the 1,2-HOPO ligand, may also become interesting alternatives for the design of Zr(iv) chelators with improved characteristics for applications in nuclear imaging with 89Zr.

SUBMITTER: Guerard F 

PROVIDER: S-EPMC5488699 | biostudies-literature | 2017 Apr

REPOSITORIES: biostudies-literature

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Investigation of the complexation of <sup>nat</sup>Zr(iv) and <sup>89</sup>Zr(iv) by hydroxypyridinones for the development of chelators for PET imaging applications.

Guérard F F   Beyler M M   Lee Y-S YS   Tripier R R   Gestin J-F JF   Brechbiel M W MW  

Dalton transactions (Cambridge, England : 2003) 20170401 14


Three hydroxypyridinone (HOPO) positional isomers - 1,2-HOPO (L1H) and its water soluble analogue (L1'H), 3,2-HOPO (L2H) and 3,4-HOPO (L3H) have been investigated for the complexation of Zr(iv). Potentiometric and UV-Vis spectrometric studies show a higher thermodynamic stability for the formation of Zr(L1')<sub>4</sub> in comparison with Zr(L2)<sub>4</sub> and Zr(L3)<sub>4</sub> as well as a higher kinetic inertness in competition studies with EDTA or Fe<sup>3+</sup> at a radiotracer concentrat  ...[more]

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