Study on dual-site inhibitors of acetylcholinesterase: Highly potent derivatives of bis- and bifunctional huperzine B

doi:10.1016/j.bmc.2006.11.009

	Study on dual-site inhibitors of acetylcholinesterase: Highly potent derivatives of bis- and bifunctional huperzine B
	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
	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
出版者	PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号	WOS:000243959100020
内容类型	期刊论文
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.