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题名: Rational design and synthesis of highly potent anti-acetylcholinesterase activity huperzine A derivatives
作者: Yan, Jian1, 2; Sun, Lirong3; Wu, Guisheng1; Yi, Ping1; Yang, Fumei4, 5; Zhou, Lin1; Zhang, Xianmin1; Li, Zhongrong1; Yang, Xiaosheng4, 5; null(罗怀容)1; null(邱明华)1
刊名: BIOORGANIC & MEDICINAL CHEMISTRY
关键词: Alzheimer's disease ; Hupzine A ; AChE ; Docking study
英文摘要: By targeting multi-active sites of acetylcholinesterase (AChE), a series of huperzine A (Hup A) derivatives with various aromatic ring groups were designed and synthesized by Schiff reaction. They were evaluated as AChE and butyrylcholinesterase (BChE) inhibitors. Results showed very significant specificity that the group of imine derivatives could inhibit TcAChE and hAChE, but no inhibitory effect on hBChE was detected. The experiment was explained by a docking study. In the docking model, we confirmed that aromatic ring of Hup A derivatives played the pi-pi stacking against aminophenol residues of AChE, and the structure-activity relationship (SAR) was discussed. (C) 2009 Elsevier Ltd. All rights reserved.
出版日期: 2009-10-01
卷号: 17, 期号:19, 页码:6937-6941
DOI标识: 10.1016/j.bmc.2009.08.017
语种: 英语
收录类别: SCI
学科分类: Biochemistry & Molecular Biology; Chemistry, Medicinal; Chemistry, Organic
ISSN号: 0968-0896
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.kib.ac.cn/handle/151853/4156
Appears in Collections:植物化学与西部植物资源持续利用国家重点实验室_期刊论文

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作者单位: 1.Chinese Acad Sci, Kunming Inst Bot, State Key Lab Phytochem & Plant Resources W China, Kunming 650204, Peoples R China
2.Chinese Acad Sci, S China Bot Garden, Guangzhou 510650, Guangdong, Peoples R China
3.So Med Univ, Sch Basic Med Sci, Guangzhou 510515, Guangdong, Peoples R China
4.Chinese Acad Sci, Guiyang 550002, Peoples R China
5.Key Lab Chem Nat Prod Guizhou Prov, Guiyang 550002, Peoples R China

Recommended Citation:
Yan, J; Sun, LR; Wu, GS; Yi, P; Yang, FM; Zhou, L; Zhang, XM; Li, ZR; Yang, XS; Luo, HR; Qiu, MH.Rational design and synthesis of highly potent anti-acetylcholinesterase activity huperzine A derivatives,BIOORGANIC & MEDICINAL CHEMISTRY,2009,17(19):6937-6941
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