Coordination Chemistry of Bifunctional Chemical Agents Designed for Applications in 64Cu PET Imaging for Alzheimer's Disease.
Inorg Chem
; 56(22): 13801-13814, 2017 Nov 20.
Article
em En
| MEDLINE
| ID: mdl-29112419
ABSTRACT
Positron emission tomography (PET) is emerging as one of the most important diagnostic tools for brain imaging, yet the most commonly used radioisotopes in PET imaging, 11C and 18F, have short half-lives, and their usage is thus somewhat limited. By comparison, the 64Cu radionuclide has a half-life of 12.7 h, which is ideal for administering and imaging purposes. In spite of appreciable research efforts, high-affinity copper chelators suitable for brain imaging applications are still lacking. Herein, we present the synthesis and characterization of a series of bifunctional compounds (BFCs) based on macrocyclic 1,4,7-triazacyclononane and 2,11-diaza[3.3](2,6)pyridinophane ligand frameworks that exhibit a high affinity for Cu2+ ions. In addition, these BFCs contain a 2-phenylbenzothiazole fragment that is known to interact tightly with amyloid ß fibrillar aggregates. Determination of the protonation constants (pKa values) and stability constants (log ß values) of these BFCs, as well as characterization of the isolated copper complexes using X-ray crystallography, electron paramagnetic resonance spectroscopy, and electrochemical studies, suggests that these BFCs exhibit desirable properties for the development of novel 64Cu PET imaging agents for Alzheimer's disease.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Compostos Aza
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Quelantes
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Compostos Radiofarmacêuticos
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Cobre
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Compostos Macrocíclicos
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Complexos de Coordenação
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Doença de Alzheimer
Limite:
Animals
Idioma:
En
Revista:
Inorg Chem
Ano de publicação:
2017
Tipo de documento:
Article
País de afiliação:
Estados Unidos