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Hafnium-Based Contrast Agents for X-ray Computed Tomography
Markus Berger1, Marcus Bauser1, Thomas Frenzel1
1Drug Discovery, Pharmaceuticals, Bayer AG , 13342 Berlin, Germany.
Inorganic Chemistry
|April 22, 2017
Abstract:
Heavy-metal-based contrast agents (CAs) offer enhanced X-ray absorption for X-ray computed tomography (CT) compared to the currently used iodinated CAs. We report the discovery of new lanthanide and hafnium azainositol complexes and their optimization with respect to high water solubility and stability. Our efforts culminated in the synthesis of BAY-576, an uncharged hafnium complex with 3:2 stoichiometry and broken complex symmetry. The superior properties of this asymmetrically substituted hafnium CA were demonstrated by a CT angiography study in rabbits that revealed excellent signal contrast enhancement.