Development of dual targeting inhibitors against aggregations of amyloid-β and tau protein

被引：45

作者：

Fuse, Shinichiro ^{[1
]}

Matsumura, Keisuke ^{[1
]}

Fujita, Yuki ^{[2
]}

Sugimoto, Hachiro ^{[2
]}

Takahashi, Takashi ^{[3
]}

机构：

[1] Tokyo Inst Technol, Dept Appl Chem, Meguro Ku, Tokyo 1528552, Japan

[2] Doshisha Univ, Grad Sch Brain Sci, Kizugawa, Kyoto 6190225, Japan

[3] Yokohama Coll Pharm, Totsuka Ku, Yokohama, Kanagawa 2450066, Japan

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2014年 / 85卷

关键词：

Alzheimer's disease; Amyloid-beta; Tau; Aggregation; Suzuki-Miyaura coupling; FLUORESCENT ORGANIC NANOPARTICLES; ALZHEIMERS-DISEASE; DYES; PEPTIDES; DESIGN;

D O I：

10.1016/j.ejmech.2014.07.095

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Aggregations of both amyloid-beta (A beta) and hyper-phosphorylated tau proteins are recognized as key pathological manifestations of Alzheimer's disease (AD). Agents that inhibit both those forms of aggregation show promise as drug candidates. Seventeen oligo heteroaromatic compounds were rapidly synthesized via a one-pot, 3- or 4-component coupling procedure. Evaluations showed that compounds E16 and E18 were the most potent inhibitors of A beta and tau aggregations (E16: IC(50)s = 0.38, 0.29 mu M against A beta, tau, respectively, E18: IC(50)s = 0.55, 0.30 mu M against A beta, tau, respectively). (C) 2014 Elsevier Masson SAS. All rights reserved.

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页码：228 / 234

页数：7

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