Oxorhenium(V) and Oxotechnetium(V) Complexes of N3S Tetradentate Ligands with a Styrylpyridyl Functional Group: Toward Imaging Agents to Assist in the Diagnosis of Alzheimer's Disease.
Inorg Chem
; 60(17): 13669-13680, 2021 Sep 06.
Article
en En
| MEDLINE
| ID: mdl-34424670
ABSTRACT
Alzheimer's disease (AD) is associated with the presence of amyloid plaques in the brain mainly comprised of aggregated forms of amyloid-ß (Aß). Molecules radiolabeled with technetium-99m that cross the blood-brain barrier (BBB) and selectively bind to Aß plaques have the potential to assist in the diagnosis of AD using single-photon emission computed tomography imaging. In this work, three new tetradentate ligands of pyridyl, amide, amine and thiol donors, featuring a styrylpyridyl group that is known to interact with amyloid plaques, were prepared. The new ligands formed charge-neutral and lipophilic complexes with the [TcâO]3+ and [ReâO]3+ motifs, and two rhenium complexes were characterized by X-ray crystallography. The rhenium(V) complexes interact with synthetic Aß1-40 and amyloid plaques on human brain tissue. Two of the new ligands were radiolabeled with 99mTc using a kit-based approach, and their biodistribution in wild-type mice was evaluated. The presence of amide donors in the tetradentate ligand increased the stability of the respective [TcâO]3+ complexes but reduced brain uptake. While the complexes were able to cross the BBB, the degree of uptake in the brain was not sufficient to justify further investigation of these complexes.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Compuestos de Organotecnecio
/
Radiofármacos
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Complejos de Coordinación
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Enfermedad de Alzheimer
Tipo de estudio:
Diagnostic_studies
Límite:
Animals
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Humans
Idioma:
En
Revista:
Inorg Chem
Año:
2021
Tipo del documento:
Article
País de afiliación:
Australia