Ferulic acid and benzothiazole dimer derivatives with high binding affinity to beta-amyloid fibrils

Abstract

New ferulic acid and benzothiazole dimer derivatives were synthesized and evaluated by in vitro competition assay using [I-125]TZDM for their specific binding affinities to A beta fibrils. In particular, 4a showed the most excellent binding affinity (K-i = 0.53 nM), compared to PIB (K-i = 0.77 nM), for benzothiazole binding sites of A beta(1-42) fibrils. This result suggests a possibility of a potential AD diagnostic probe for detection of A beta fibrils. (C) 2007 Elsevier Ltd. All rights reserved.