Design, synthesis, and acetylcholinesterase inhibitory activity of novel coumarin analogues
Design, synthesis, and acetylcholinesterase inhibitory activity of novel coumarin analogues
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DOI：
10.1016/j.bmc.2008.07.068
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发表时间：
2008-09-01
影响因子：
3.5
通讯作者：
Kong, Ling-Yi
中科院分区：
文献类型：
--
作者：
Zhou, Xiang;Wang, Xiao-Bing;Kong, Ling-Yi
设计合成了3个系列（A-C系列）含苯基哌嗪取代的香豆素类化合物，研究其治疗阿尔茨海默病的潜力。以多奈哌齐为参比化合物，采用Ellmann法测定了它们对新鲜制备的电鳗乙酰胆碱酯酶（AChE）的抑制活性。药理学研究和初步构效关系表明，3位和/或4位取代的香豆素类化合物具有与参比化合物平行的抗AchE活性。(C)2008爱思唯尔有限公司保留所有权利。
Three series (series A-C) of coumarin analogues with phenylpiperazine functions as substitution were designed and synthesized for studying their potential for treating Alzheimer's (AD) disease. Their anticholinesterase activities were assayed according to Ellmann's method against freshly prepared acetylcholinesterase (AChE) from Electrophorus electricus using donepezil as the reference compound. Pharmacological study and preliminary structure-activity relationships showed that coumarins with substitution on positions 3 and/or 4 have parallel anti-AchE activities compared with the reference compound. (C) 2008 Elsevier Ltd. All rights reserved.