化学
乙酰胆碱酯酶
IC50型
立体化学
酶
阿切
药理学
生物化学
体外
医学
作者
Sarawalee Arunkhamkaew,Anan Athipornchai,Nuttapon Apiratikul,Apichart Suksamrarn,Vachiraporn Ajavakom
标识
DOI:10.1016/j.bmcl.2013.03.069
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 μM which was more active than the approved drug galanthamine (IC50 = 1.45 ± 0.04 μM).
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