Rational design and synthesis of highly potent anti-acetylcholinesterase activity huperzine A derivatives

doi:10.1016/j.bmc.2009.08.017

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	Rational design and synthesis of highly potent anti-acetylcholinesterase activity huperzine A derivatives
	Yan, Jian 1,2; Sun, Lirong 3; Wu, Guisheng1 ; Yi, Ping 1; Yang, Fumei 4,5; Zhou, Lin 1; Zhang, Xianmin 1; Li, Zhongrong 1; Yang, Xiaosheng 4,5; Luo, Huairong1
刊名	BIOORGANIC & MEDICINAL CHEMISTRY
	2009-10-01
卷号	17 期号:19 页码:6937-6941
关键词	Alzheimer's Disease Hupzine a Ache Docking Study
ISSN号	0968-0896
DOI	10.1016/j.bmc.2009.08.017
文献子类	Article
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.
学科主题	Biochemistry & Molecular Biology ; Chemistry, Medicinal ; Chemistry, Organic
WOS关键词	ACETYLCHOLINESTERASE INHIBITORS ; ALZHEIMERS-DISEASE ; ANTICHOLINESTERASE ACTIVITY ; SITE GORGE ; CHOLINESTERASE INHIBITOR ; TORPEDO-CALIFORNICA ; ANALOGS ; GALANTHAMINE ; AGENT ; DRUGS
WOS研究方向	Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
语种	英语
WOS记录号	WOS:000269724600017
资助机构	Program of Promoting Development for Guizhou, China [Qian-01-2005-01]; CAS ; National Sciences of Yunnan, China [2005C0010Z]; Chinese Academy of Sciences [KSCX2-YW-G-038]; National Natural Science Foundation of China [30772636]
公开日期	2012-03-21
内容类型	期刊论文
源URL	[http://ir.kib.ac.cn:8080/handle/151853/4156]
专题	昆明植物研究所_植物化学与西部植物资源持续利用国家重点实验室
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
推荐引用方式 GB/T 7714	Yan, Jian,Sun, Lirong,Wu, Guisheng,et al. Rational design and synthesis of highly potent anti-acetylcholinesterase activity huperzine A derivatives[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2009,17(19):6937-6941.
APA	Yan, Jian.,Sun, Lirong.,Wu, Guisheng.,Yi, Ping.,Yang, Fumei.,...&Qiu, Minghua.(2009).Rational design and synthesis of highly potent anti-acetylcholinesterase activity huperzine A derivatives.BIOORGANIC & MEDICINAL CHEMISTRY,17(19),6937-6941.
MLA	Yan, Jian,et al."Rational design and synthesis of highly potent anti-acetylcholinesterase activity huperzine A derivatives".BIOORGANIC & MEDICINAL CHEMISTRY 17.19(2009):6937-6941.