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
收藏
页码：4148 / 4153
页数：6
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