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
收藏
页码：5576 / 5582
页数：7
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