| 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 | |
| Source Publication | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| ISSN | 0968-0896 |
| Volume | 17Issue:19Pages:6937-6941 |
| Abstract | 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. |
| Keyword | Alzheimer's Disease Hupzine a Ache Docking Study |
| Subject Area | Biochemistry & Molecular Biology ; Chemistry, Medicinal ; Chemistry, Organic |
| DOI | 10.1016/j.bmc.2009.08.017 |
| Indexed By | SCI |
| Language | 英语 |
| WOS ID | WOS:000269724600017 |
| Citation statistics | |
| Document Type | 期刊论文 |
| Identifier | http://ir.kib.ac.cn/handle/151853/4156 |
| Collection | 植物化学与西部植物资源持续利用国家重点实验室 |
| Affiliation | 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 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. |
| Files in This Item: | Download All | |||||
| File Name/Size | DocType | Version | Access | License | ||
| 201112280017.pdf（368KB） | 开放获取 | -- | View Download | |||
Items in the repository are protected by copyright, with all rights reserved, unless otherwise indicated.
Edit Comment