Novel racemic tetrahydrocurcuminoid dihydropyrimidinone analogues as potent acetylcholinesterase inhibitors

被引：37
作者：
Arunkhamkaew, Sarawalee
Athipornchai, Anan
Apiratikul, Nuttapon
Suksamrarn, Apichart
Ajavakom, Vachiraporn [1 ]
机构：
[1] Ramkhamhang Univ, Fac Sci, Dept Chem, Bangkok 10240, Thailand
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2013年 / 23卷 / 10期
关键词：
Alzheimer's disease; Acetylcholinesterase inhibitor; Curcumin; Dihydropyrimidinone; SOLVENT-FREE CONDITIONS; ALZHEIMERS-DISEASE; ANTIMICROBIAL ACTIVITY; BIGINELLI REACTION; CURCUMIN; DERIVATIVES; DESIGN; AGENTS; 3,4-DIHYDROPYRIMIDINONES; 3-COMPONENT;
D O I：
10.1016/j.bmcl.2013.03.069
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The synthesis of racemic tetrahydrocurcumin- (THC-), tetrahydrodemethoxycurcumin- (THDC-) and tetrahydrobisdemethoxycurcumin- (THBDC-) dihydropyrimidinone (DHPM) analogues was achieved by utilizing the multi-component Biginelli reaction in the presence of copper sulphate as a catalyst. The evaluation of acetylcholinesterase inhibitors for Alzheimer's disease of these compounds showed that they exhibited higher inhibitory activity than their parent analogues. THBDC-DHPM demonstrated the most potent inhibitory activity with an IC50 value of 1.34 +/- 0.03 mu M which was more active than the approved drug galanthamine (IC50 = 1.45 +/- 0.04 mu M). (C) 2013 Elsevier Ltd. All rights reserved.
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收藏
页码：2880 / 2882
页数：3
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