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 ...