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Quick assembly of 1, 4-diphenyltriazoles as probes targeting β-amyloid aggregates in Alzheimer's disease

…, MP Kung, C Hou, S Oya, HF Kung

文献索引:Qu, Wenchao; Kung, Mei-Ping; Hou, Catherine; Oya, Shunichi; Kung, Hank F. Journal of Medicinal Chemistry, 2007 , vol. 50, # 14 p. 3380 - 3387

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被引用次数: 74

摘要

Accumulation of β-amyloid aggregates (Aβ) in the brain is linked to the pathogenesis of Alzheimer's disease (AD). We report a novel approach for producing 1, 4-diphenyltriazoles as probes for targeting Aβ aggregates in the brain. The imaging probes, a series of substituted tricyclic 1, 4-diphenyltriazoles showing excellent binding affinities to Aβ aggregates (K i= 4-30 nM), were conveniently assembled by “click chemistry.” Two ...