Study on dual-site inhibitors of acetylcholinesterase: Highly potent derivatives of bis- and bifunctional huperzine B
文献类型：期刊论文
| 作者 | He, Xu-Chang; Feng, Song; Wang, Zhi-Fei; Shi, Yufang; Zheng, Suxin; Xia, Yu; Jiang, Hualiang ; Tang, Xi-Can; Bai, Donglu
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2007-02-01 |
| 卷号 | 15期号:3页码:1394-1408 |
| 关键词 | Huperzine B acetylcholinesterase Alzheimer's disease dual-site binding inhibitors |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2006.11.009 |
| 文献子类 | Article |
| 英文摘要 | Natural (-)-huperzine B (HupB), isolated from Chinese medicinal herb, displayed moderate inhibitory activity of acetylcholinesterase (AChE). Based on the active dual-site of AChE, a series of novel derivatives of bis- and bifunctional HupB were designed and synthesized. The AChE inhibition potency of most derivatives of HupB was enhanced about 2-3 orders of magnitude as compared with the parental HupB. Among bis-HupB derivatives, 12h exhibited the most potent in the AChE inhibition and has been evaluated for its pharmacological actions in vivo on ChE inhibition, cognitive enhancement, and neuroprotection. The docking study on the bis-HupB derivatives 12 series with TcAChE has demonstrated that the ligands bound to the dual-site of the enzyme in different level. (c) 2006 Elsevier Ltd. All rights reserved. |
| WOS关键词 | ALZHEIMERS-DISEASE ; TORPEDO-CALIFORNICA ; BINDING ; DOCKING ; PROTEIN ; DRUGS ; MICE |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000243959100020 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/273333]  |
| 专题 | 药物化学研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | He, Xu-Chang |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, Dept Synth Drugs, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | He, Xu-Chang,Feng, Song,Wang, Zhi-Fei,et al. Study on dual-site inhibitors of acetylcholinesterase: Highly potent derivatives of bis- and bifunctional huperzine B[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2007,15(3):1394-1408. |
| APA | He, Xu-Chang.,Feng, Song.,Wang, Zhi-Fei.,Shi, Yufang.,Zheng, Suxin.,...&Bai, Donglu.(2007).Study on dual-site inhibitors of acetylcholinesterase: Highly potent derivatives of bis- and bifunctional huperzine B.BIOORGANIC & MEDICINAL CHEMISTRY,15(3),1394-1408. |
| MLA | He, Xu-Chang,et al."Study on dual-site inhibitors of acetylcholinesterase: Highly potent derivatives of bis- and bifunctional huperzine B".BIOORGANIC & MEDICINAL CHEMISTRY 15.3(2007):1394-1408. |
入库方式： OAI收割
来源：上海药物研究所
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