Synthesis of donepezil-based multifunctional agents for the treatment of Alzheimer's disease

被引：23

作者：

Yerdelen, Kadir Ozden ^{[1
]}

Koca, Mehmet ^{[1
]}

Anil, Baris ^{[2
]}

Sevindik, Handan ^{[3
]}

Kasap, Zeynep ^{[1
]}

Halici, Zekai ^{[4
]}

Turkaydin, Kubra ^{[1
]}

Gunesacar, Gulsen ^{[1
]}

机构：

[1] Ataturk Univ, Fac Pharm, Dept Pharmaceut Chem, TR-25240 Erzurum, Turkey

[2] Ataturk Univ, Dept Organ Chem, Fac Pharm, TR-25240 Erzurum, Turkey

[3] Ataturk Univ, Dept Pharmacognosy, Fac Pharm, TR-25240 Erzurum, Turkey

[4] Ataturk Univ, Dept Pharmacol, Fac Med, TR-25240 Erzurum, Turkey

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2015年 / 25卷 / 23期

关键词：

Donepezil; Amyloid beta; Alzheimer; AChE; BuChE; AMYLOID-BETA; ANTICHOLINESTERASE ACTIVITY; ACETYLCHOLINESTERASE; INHIBITORS; DOCKING; AGGREGATION; ANALOGS; ACHE; BUTYRYLCHOLINESTERASE; 2-BUTENEDIAMIDE;

D O I：

10.1016/j.bmcl.2015.10.051

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Amyloid beta (A beta) and cholinesterase enzymes (AChE, BuChE) are important biological targets for the effective treatment of Alzheimer's disease. In this study, the aim was to synthesize new donepezil-like secondary amide compounds that display a potent inhibition of cholinesterases and A beta with antioxidant and metal chelation abilities. All test compounds showed activities against both ChEs and beta(1-42) inhibition. The most encouraging compound, 20, is an AChE inhibitor with high anti-aggregation activity (55.3%). Based on the results, compound 20 may be a promising structure in further research for new anti-Alzheimer's agents. (C) 2015 Elsevier Ltd. All rights reserved.

引用

页码：5576 / 5582

页数：7

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