Synthesis and evaluation of benzofuran-2-yl(phenyl)methanone derivatives as ligands for β-amyloid plaques

被引：22

作者：

Cui, Mengchao ^{[1
,2
]}

Ono, Masahiro ^{[1
]}

Kimura, Hiroyuki ^{[1
]}

Liu, Boli ^{[2
]}

Saji, Hideo ^{[1
]}

机构：

[1] Kyoto Univ, Grad Sch Pharmaceut Sci, Sakyo Ku, Kyoto 6068501, Japan

[2] Beijing Normal Univ, Key Lab Radiopharmaceut, Minist Educ, Coll Chem, Beijing 100875, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2011年 / 19卷 / 13期

关键词：

Alzheimer's disease; beta-Amyloid; Imaging agent; Binding assay; Autoradiography; ALZHEIMERS-DISEASE; IMAGING AGENTS; BRAIN; PROBES; CHALCONES; BIODISTRIBUTION; RADIOLIGAND; DOSIMETRY; AURONES;

D O I：

10.1016/j.bmc.2011.04.049

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of benzofuran-2-yl(phenyl)methanone derivatives were synthesized and evaluated as novel probes for beta-amyloid plaques. These derivatives were produced by a Rap-Stoermer condensation reaction. Compounds with a N,N-dimethylamino group displayed high affinity for A beta(1-42) aggregates with K(i) values in the nanomolar range. Autoradiography with brain sections of AD model mice (APP/PS1) revealed that a radioiodinated probe, [(125)I]10, labeled beta-amyloid plaques selectively and displayed good brain uptake (3.53% ID/g) at 2 min. The results suggest that benzofuran-2-yl(phenyl) methanone derivatives should be investigated further as potential probes for detecting beta-amyloid plaques in the AD brain. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：4148 / 4153

页数：6

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