Benzothiazole Schiff-bases as potential imaging agents for β-amyloid plaques in Alzheimer’s disease

Autor:	Zhenzhen Zhao, Lin Zhou, Haoshu Wang, Changsheng Gan
Rok vydání:	2012
Předmět:	chemistry.chemical_compound Benzothiazole Amyloid Chemistry β amyloid Organic Chemistry Fluorescent staining Early detection General Pharmacology Toxicology and Pharmaceutics Ligand (biochemistry) Molecular biology In vitro Binding affinities
Zdroj:	Medicinal Chemistry Research. 22:4069-4074
ISSN:	1554-8120 1054-2523
DOI:	10.1007/s00044-012-0416-0
Popis:	A series of benzothiazole Schiff-bases as potential diagnostic imaging agents targeting β-amyloid (Aβ) plaques in Alzheimer’s disease (AD) were synthesized and evaluated. When in vitro binding studies using AD homogenate with [125I] 6-iodo-2-(4′-dimethyl- amino)-phenyl-imidazo[1,2-α]pyridine ([125I]IMPY) as the reference ligand were carried out with the derivatives, the compounds showed high to low binding affinities for AD homogenate at the K i values ranged from 4.38 to 514.65 nM, depending on the substitution on the phenyl ring. Fluorescent staining in vitro showed that one compound with a N,N-dimethylamino group intensely stained Aβ plaques within brain sections of postmortem AD patients. The results strongly suggest that these derivatives are worthy of further study and may be a useful amyloid imaging agents for early detection of amyloid plaques in the brain of AD.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::35dec95be3379204720775836b0376c2 https://doi.org/10.1007/s00044-012-0416-0 Zobrazit plný text záznamu Full text from SpringerLink