Novel anilinophthalimide derivatives as potential probes for β-amyloid plaque in the brain

XH Duan, JP Qiao, Y Yang, MC Cui, JN Zhou…

Index: Duan, Xin-Hong; Qiao, Jin-Ping; Yang, Yang; Cui, Meng-Chao; Zhou, Jiang-Ning; Liu, Bo-Li Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 3 p. 1337 - 1343

Full Text: HTML

Citation Number: 11

Abstract

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, ...