Development of novel β-amyloid probes based on 3, 5-diphenyl-1, 2, 4-oxadiazole

M Ono, M Haratake, H Saji, M Nakayama

Index: Ono, Masahiro; Haratake, Mamoru; Saji, Hideo; Nakayama, Morio Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 14 p. 6867 - 6872

Full Text: HTML

Citation Number: 49

Abstract

In the search for novel probes for the imaging in vivo of β-amyloid plaques in Alzheimer's disease (AD) brain, we have synthesized and evaluated a series of 3, 5-diphenyl-1, 2, 4- oxadiazole (DPOD) derivatives. The affinity for β-amyloid plaques was assessed by an in vitro-binding assay using pre-formed synthetic Aβ42 aggregates. The new series of DPOD derivatives showed excellent affinity for Aβ aggregates with Ki values ranging from 4 to ...