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

被引：33

作者：

Byeon, Seong Rim

Jin, Yun Jung

Lim, Soo Jeong

Lee, Ji Hoon

Yoo, Kyung Ho

Shin, Kye Jung

Oh, Seung Jun

Kim, Don Jin

机构：

[1] Korea Inst Sci & Technol, Ctr Chemoinformat Res, Seoul 130650, South Korea

[2] Asan Med Ctr, Dept Nucl Med, Seoul 138736, South Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 14期

关键词：

ferulic acid dimer; benzothiazole dimer; A beta fibrils; AD diagnostic probe;

D O I：

10.1016/j.bmcl.2007.04.079

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：4022 / 4025

页数：4

共 26 条

[1] Pinpointing plaques with PIB [J].