Rational design and synthesis of highly potent anti-acetylcholinesterase activity huperzine A derivatives
Yan, Jian1,2; Sun, Lirong3; Wu, Guisheng1; Yi, Ping1; Yang, Fumei4,5; Zhou, Lin1; Zhang, Xianmin1; Li, Zhongrong1; Yang, Xiaosheng4,5; Luo, Huairong1; Qiu, Minghua1
2009-10-01
发表期刊BIOORGANIC & MEDICINAL CHEMISTRY
ISSN0968-0896
卷号17期号:19页码:6937-6941
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.
关键词Alzheimer's Disease Hupzine a Ache Docking Study
资助信息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]
收录类别SCI
语种英语
引用统计
文献类型期刊论文
条目标识符http://ir.kib.ac.cn/handle/151853/4156
专题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
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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.
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