Design, synthesis, and structure-activity relationship of novel thiophene derivatives for β-amyloid plaque imaging

被引：45

作者：

Chandra, R

Kung, MP

Kung, HF

机构：

[1] Univ Penn, Dept Radiol, Philadelphia, PA 19104 USA

[2] Univ Penn, Dept Pharmacol, Philadelphia, PA 19104 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 05期

关键词：

in vitro binding; PET imaging; Alzheimer's disease;

D O I：

10.1016/j.bmcl.2005.11.055

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Novel 2,5-diphenylthiophene derivatives were synthesized and structure activity relationship with regard to A beta plaque binding was studied. Binding affinities of these compounds were found to range from 3.9 to >1000 nM, depending on the substitution patterns on the phenyl ring. The fluoroethyl-substituted thiophene derivatives showed excellent binding affinities. These compounds may be useful for the development of novel PET tracers for the imaging of beta-amyloid plaques in the brain of patients with Alzheimer's disease. (C) 2005 Elsevier Ltd. All rights reserved.

引用

收藏

页码：1350 / 1352

页数：3

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