Novel coumarin derivatives bearing N-benzyl pyridinium moiety: Potent and dual binding site acetylcholinesterase inhibitors
Novel coumarin derivatives bearing N-benzyl pyridinium moiety: Potent and dual binding site acetylcholinesterase inhibitors
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DOI：
10.1016/j.bmc.2012.08.052
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发表时间：
2012-12-15
影响因子：
3.5
通讯作者：
Shafiee, Abbas
中科院分区：
文献类型：
--
作者：
Alipour, Masoumeh;Khoobi, Mehdi;Shafiee, Abbas
合成了一系列新型苄基吡啶基香豆素衍生物，并对其乙酰胆碱酯酶（AChE）和丁酰胆碱酯酶（BuChE）抑制剂进行了生物活性评价。采用比色Ellman法测定了合成化合物的酶抑制活性。结果表明，化合物3e、3h、3l、3r和3s的活性均高于盐酸多奈哌齐。这些系列中的大多数化合物具有纳摩尔范围的IC 50，其中化合物3r（IC 50 = 0.11 nM）是对乙酰胆碱酯酶最具活性的化合物。(C)2012爱思唯尔有限公司保留所有权利。
A novel series of coumarin derivatives linked to benzyl pyridinium group were synthesized and biologically evaluated as inhibitors of both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). The enzyme inhibitory activity of synthesized compounds was measured using colorimetric Ellman's method. It was revealed that compounds 3e, 3h, 3l, 3r and 3s have shown higher activity compared with donepezil hydrochloride as standard drug. Most of the compounds in these series had nanomolar range IC50 in which compound 3r (IC50 = 0.11 nM) was the most active compound against acetylcholinesterase enzyme. (C) 2012 Elsevier Ltd. All rights reserved.