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

…, YJ Jin, SJ Lim, JH Lee, KH Yoo, KJ Shin, SJ Oh…

Index: Byeon, Seong Rim; Jin, Yun Jung; Lim, Soo Jeong; Lee, Ji Hoon; Yoo, Kyung Ho; Shin, Kye Jung; Oh, Seung Jun; Kim, Dong Jin Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 14 p. 4022 - 4025

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Citation Number: 25

Abstract

New ferulic acid and benzothiazole dimer derivatives were synthesized and evaluated by in vitro competition assay using [125I] TZDM for their specific binding affinities to Aβ fibrils. In particular, 4a showed the most excellent binding affinity (Ki= 0.53 nM), compared to PIB (Ki= 0.77 nM), for benzothiazole binding sites of Aβ1–42 fibrils. This result suggests a possibility of a potential AD diagnostic probe for detection of Aβ fibrils.