Novel racemic tetrahydrocurcuminoid dihydropyrimidinone analogues as potent acetylcholinesterase inhibitors
Novel racemic tetrahydrocurcuminoid dihydropyrimidinone analogues as potent acetylcholinesterase inhibitors
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DOI：
10.1016/j.bmcl.2013.03.069
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发表时间：
2013-05-15
影响因子：
2.7
通讯作者：
Ajavakom, Vachiraporn
中科院分区：
文献类型：
--
作者：
Arunkhamkaew, Sarawalee;Athipornchai, Anan;Ajavakom, Vachiraporn
以硫酸铜为催化剂，利用多组分 Biginelli 反应合成了外消旋四氢姜黄素 (THC-)、四氢去甲氧基姜黄素 (THDC-) 和四氢双去甲氧基姜黄素 (THBDC-) 二氢嘧啶酮 (DHPM) 类似物。对这些化合物的乙酰胆碱酯酶抑制剂对阿尔茨海默病的评估表明，它们比其母体类似物表现出更高的抑制活性。 THBDC-DHPM 表现出最有效的抑制活性，IC50 值为 1.34 +/- 0.03 muM，比批准的药物加兰他敏 (IC50 = 1.45 +/- 0.04 muM) 活性更高。 (C) 2013 Elsevier Ltd. 保留所有权利。
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.