Fluorinated benzofuran derivatives for PET imaging of β-amyloid plaques in Alzheimer's disease brains

Y Cheng, M Ono, H Kimura, S Kagawa…

Index: Cheng, Yan; Ono, Masahiro; Kimura, Hiroyuki; Kagawa, Shinya; Nishii, Ryuichi; Kawashima, Hidekazu; Saji, Hideo ACS Medicinal Chemistry Letters, 2010 , vol. 1, # 7 p. 321 - 325

Full Text: HTML

Citation Number: 23

Abstract

A series of fluorinated benzofuran derivatives as potential tracers for positron emission tomography (PET) targeting β-amyloid plaques in the brains of patients with Alzheimer's disease (AD) were synthesized and evaluated. The derivatives were produced using an intramolecular Wittig reaction. In experiments in vitro, all displayed high affinity for Aβ (1− 42) aggregates with K i values in the nanomolar range. Radiofluorinated 17,[18F] 17, in ...