A group of novel 4, 5-dianilinophthalimide derivatives has been synthesized in this study for potential use as β-amyloid (Aβ) plaque probes. Staining of hippocampus tissue sections from Alzheimer's disease (AD) brain with the representative compound 9 indicated selective labeling of it to Aβ plaques. The binding affinity of radioiodinated [125I] 9 for AD brain homogenates was 0.21 nM (Kd), and of other derivatives ranged from 0.9 to 19.7 nM, ...