Inhibition of acetylcholinesterase, β-amyloid aggregation, and NMDA receptors in Alzheimer's disease:: A promising direction for the multi-target-directed ligands gold rush

被引：191

作者：

Rosini, Michela ^{[1
]}

Simoni, Elena ^{[1
]}

Bartolini, Manuela ^{[1
]}

Cavalli, Andrea ^{[1
]}

Ceccarini, Luisa ^{[1
]}

Pascu, Nicoleta ^{[3
]}

McClymont, David W. ^{[3
]}

Tarozzi, Andrea ^{[2
]}

Bolognesi, Maria L. ^{[1
]}

Minarini, Anna ^{[1
]}

Tumiatti, Vincenzo ^{[1
]}

Andrisano, Vincenza ^{[1
]}

Mellor, Ian R. ^{[3
]}

Melchiorre, Carlo ^{[1
]}

机构：

[1] Univ Bologna, Dept Pharmaceut Sci, I-40126 Bologna, Italy

[2] Univ Bologna, Dept Pharmacol, I-40126 Bologna, Italy

[3] Univ Nottingham, Sch Biol, Nottingham NG7 2RD, England

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 51卷 / 15期

关键词：

D O I：

10.1021/jm800577j

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Alzheimer's disease (AD) is a multifactorial syndrome with several target proteins contributing to its etiology. To confront AD, an innovative strategy is to design single chemical entities able to simultaneously modulate more than one target. Here, we present compounds that inhibit acety1cholinesterase and NMDA receptor activity. Furthermore, these compounds inhibit AChE-induced AP aggregation and display antioxidant properties, emerging as lead candidates for treating AD.

引用

页码：4381 / 4384

页数：4

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