Novel racemic tetrahydrocurcuminoid dihydropyrimidinone analogues as potent acetylcholinesterase inhibitors

被引：41

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：

100705 [微生物与生化药学];

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.

引用

页码：2880 / 2882

页数：3

共 41 条

[1]

Inhibitory effect of curcuminoids on acetylcholinesterase activity and attenuation of scopolamine-induced amnesia may explain medicinal use of turmeric in Alzheimer's disease [J].