Syntheses and evaluation of fluorinated benzothiazole anilines as potential tracers for β-amyloid plaques in Alzheimer's disease

Autor:	Duanzhi Yin, Lan Zhang, Ming-Qiang Zheng, Yongxian Wang, Jin-Ping Qiao
Rok vydání:	2008
Předmět:	Stereochemistry Chemistry Organic Chemistry Radiosynthesis Biochemistry In vitro Inorganic Chemistry chemistry.chemical_compound Benzothiazole β amyloid In vivo Proton NMR Environmental Chemistry Physical and Theoretical Chemistry Pet tracer
Zdroj:	Journal of Fluorine Chemistry. 129:210-216
ISSN:	0022-1139
DOI:	10.1016/j.jfluchem.2007.11.005
Popis:	[11C]2-(4′-(Methylamino)phenyl)-6-hydroxybenzothiazole ([11C]PIB) is a most potential PET tracer for detecting the β-amyloid plaques in Alzheimer's disease. Here the syntheses of three fluorinated PIB, namely 2-(4′-(methylamino)phenyl)-6-fluoroethoxybenzothiazole (O-FEt-PIB), 2-(4′-(methylamino)phenyl)-6-fluoro-benzothiazole (F-N-Me) and 2-(4′-(dimethylamino)phenyl)-6-fluorobenzo-thiazole (F-N,N-Me), and the radiosynthesis of one corresponding 18F-labeled PIB compound, [18F]O-FEt-PIB, as well as their in vitro/in vivo biological characters were reported. The structures of the products were confirmed by IR, 1H NMR, EI/ESI-MS, elemental analysis and HRMS techniques. The radiolabeled product was characterized by radio-TLC and radio-HPLC and purified by semi-preparative radio-HPLC. The suitable biological characters showed these tracers were potential to be developed as probes for detecting β-amyloid plaques in Alzheimer's disease.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::0c1dcb5abc01ef9a67ac94611b423c36 https://doi.org/10.1016/j.jfluchem.2007.11.005 Zobrazit plný text záznamu Full Text from ScienceDirect