Novel 18F-labeled dibenzylideneacetone derivatives as potential positron emission tomography probes for in vivo imaging of β-amyloid plaques

A series of dibenzylideneacetones were synthesized and evaluated as imaging probes for beta-amyloid plaques. They displayed high binding affinity to A beta(1-42) aggregates (K-i = 6.4 for 8, K-i = 3.0 for 9), and the high binding were confirmed by in vitro autoradiography with AD human and transgenic mouse brain sections. Two of them were selected for F-18-labeling directly on the benzene ring. In biodistribution experiments, [F-18]8 and [F-18]9 displayed high initial uptakes (9.29 +/- 0.41 and 5.38 +/- 0.68% ID/g) and rapid washouts from the normal brain (brain(2) (min)/brain(60) (min) ratios of 21.6 and 13.4). These preliminary results suggest that [F-18]8 and [F-18]9 may be used as potential PET imaging agents for the detection of A beta plaques in the brain. (C) 2014 Elsevier Masson SAS. All rights reserved.