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

文献索引：Bioorg. Med. Chem. Lett. 17 , 4022, (2007)

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摘要

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.