Structure-activity relationship of chalcones and related derivatives as ligands for detecting of beta-amyloid plaques in the brain.
Bioorganic & medicinal chemistry 2007 Jul 4; 15(19):6388-96
Ono M M, Hori M M, Haratake M M, Tomiyama T T, Mori H H, Nakayama M M
Department of Hygienic Chemistry, Graduate School of Biomedical Sciences, Nagasaki University, 1-14
A series of novel chalcones and their related derivatives were synthesized and evaluated as beta-amyloid imaging probes. In the structure-activity relationship of binding affinities to synthetic Abeta(1-42) aggregates, compound 14 displayed the highest binding affinity in vitro. beta-Amyloid plaques in the Alzheimer's model mouse brain were visualized with 14. In biodistribution studies using normal mice, [(125)I]14 showed good brain uptake (2.56% ID/g, 2min postinjection) and rapid washout from the brain (0.21% ID/g, 60min postinjection). These results suggest that [(125)I]14 should be further investigated as a potentially useful beta-amyloid imaging probe.