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Synthesis and docking studies of alkylene-linked dimers of (-)-huperzine A

文献类型：期刊论文

作者Jin, GY; Luo, XM; He, XC; Jiang, HL; Zhang, HY; Bai, DL
刊名ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH
出版日期2003
卷号53期号:11页码:753-757
关键词acetylcholinesterase, inhibition (-)-huperzine A, alkylene-linked dimers docking studies
ISSN号0004-4172
文献子类Article
英文摘要(-)-Huperzine A (5, HupA), an alkaloid isolated from the herb Huperzia serrata, is a potent, selective and reversible acetylcholinesterase (AchE) inhibitor. Based on the hypothesis with respect to two binding sites in the active gorge of AChE and the good example of bis-tacrine, it was predicted from the docking studies of alkylene-linked dimers of HupA that dimers 6 (n = 5, 7, 9) might have good AChE inhibitory activity. Therefore, six dimers with 7-12 methylene units as tethers were thus prepared. It was found that these dimers; were less potent than HupA in inhibition of AChE. The difference of the inhibitory potency between these dimers is coincident with the results of the docking studies.
WOS关键词ALZHEIMERS-DISEASE ; HIGHLY POTENT ; BIS-THA ; ACETYLCHOLINESTERASE ; INHIBITORS ; HUPERZINE
WOS研究方向Pharmacology & Pharmacy ; Chemistry
语种英语
WOS记录号WOS:000187179500001
出版者ECV-EDITIO CANTOR VERLAG MEDIZIN NATURWISSENSCHAFTEN
源URL[http://119.78.100.183/handle/2S10ELR8/274277]  
专题院士及顾问专家
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Bai, DL
作者单位Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai Inst Biol Sci, State Key Lab Drug Res, Shanghai 20203, Peoples R China
推荐引用方式
GB/T 7714		 Jin, GY,Luo, XM,He, XC,et al. Synthesis and docking studies of alkylene-linked dimers of (-)-huperzine A[J]. ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH,2003,53(11):753-757.
APA Jin, GY,Luo, XM,He, XC,Jiang, HL,Zhang, HY,&Bai, DL.(2003).Synthesis and docking studies of alkylene-linked dimers of (-)-huperzine A.ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH,53(11),753-757.
MLA Jin, GY,et al."Synthesis and docking studies of alkylene-linked dimers of (-)-huperzine A".ARZNEIMITTEL-FORSCHUNG-DRUG RESEARCH 53.11(2003):753-757.

入库方式： OAI收割

来源：上海药物研究所

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