Multi-target-directed coumarin derivatives: hAChE and BACE1 inhibitors as potential anti-Alzheimer compounds

被引：209

作者：

Piazzi, Lorna ^{[1
]}

Cavalli, Andrea ^{[1
]}

Colizzi, Francesco ^{[1
]}

Belluti, Federica ^{[1
]}

Bartolini, Manuela ^{[1
]}

Mancini, Francesca ^{[1
]}

Recanatini, Maurizio ^{[1
]}

Andrisano, Vincenza ^{[1
]}

Rampa, Angela ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 01期

关键词：

D O I：

10.1016/j.bmcl.2007.09.100

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The complex etiology of Alzheimer's disease (AD) prompts scientists to develop multifunctional compounds to combat causes and symptoms of such neurodegeneration. To this aim we designed, synthesized, and tested a series of compounds by introducing halophenylalkylamidic functions on the scaffold of AP2238, which is a dual binding site acetylcholinesterase inhibitor. The inhibitory activity was successfully extended to the beta-site amyloid precursor protein cleavage enzyme, leading to the discovery of a potent inhibitor of this enzyme (3) and affording multifunctional compounds (2, 6, 8) for the treatment of AD. (c) 2007 Published by Elsevier Ltd.

引用

页码：423 / 426

页数：4

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