Bioorganic & Medicinal Chemistry Letters 2007-07-15

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

Seong Rim Byeon, Yun Jung Jin, Soo Jeong Lim, Ji Hoon Lee, Kyung Ho Yoo, Kye Jung Shin, Seung Jun Oh, Dong Jin Kim

Index: Bioorg. Med. Chem. Lett. 17 , 4022, (2007)

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Abstract

New ferulic acid and benzothiazole dimer derivatives were synthesized and evaluated by in vitro competition assay using [(125)I]TZDM for their specific binding affinities to Abeta 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 Abeta(1-42) fibrils. This result suggests a possibility of a potential AD diagnostic probe for detection of Abeta fibrils.