Benzothiazole Schiff-bases as potential imaging agents for β-amyloid plaques in Alzheimer’s disease
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- Gan, C., Zhou, L., Zhao, Z. et al. Med Chem Res (2013) 22: 4069. doi:10.1007/s00044-012-0416-0
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 Ki 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.