兰州大学机构库 >化学化工学院
Synthesis and structure-activity relationship of nuciferine derivatives as potential acetylcholinesterase inhibitors
Yang, ZD; Song, ZW; Xue, WW; Sheng, J; Shu, ZM; Shi, Y; Liang, JB; Yao, XJ(姚小军); Yang, ZD (reprint author), Lanzhou Univ Technol, Sch Life Sci & Engn, Lanzhou 730050, Gansu, Peoples R China.
收录类别SCIE
2014-06
发表期刊MEDICINAL CHEMISTRY RESEARCH
卷号23期号:6
出版者SPRINGER
出版地NEW YORK
摘要Acetylcholinesterase inhibitors (AChEIs) are currently the best available pharmacotherapy for Alzheimer patients, but because of bioavailability issues, there is still great interest in discovering better AChEIs. The aporphine alkaloid is an important class of natural products, which shows diverse biological activity, such as acetylcholinesterase inhibitory activity. To find new lead AChEIs compounds, eight aporphine alkaloids were synthesized by O-dealkylation, N-dealkylation, and ring aromatization reactions using nuciferine as raw material. The anti-acetylcholinesterase activity of synthesized compounds was measured using modified Ellman's method. The results showed that some synthesized compounds exhibited higher affinity to AChE than the parent compound nuciferine. Among these compounds, 1,2-dihydroxyaporphine (2) and dehydronuciferine (5) were the most active compounds (IC50 = 28 and 25 mu g/mL, respectively). Preliminary analysis of structure-activity relationships suggested that aromatization of the C ring, the presence of the alkoxyl group at C1 and the hydroxy group at C2 position as well as the alkyl substituent at the N atom were favorable to the acetylcholinesterase inhibition. Molecular docking was also applied to predict the binding modes of compounds 1, 2, and 9 into the huperzine A binding site of AChE.
关键词Aporphine alkaloids Acetylcholinesterase inhibitors Structure-activity relationships
作者部门[Yang, Zhongduo;
Song, Zhuwen;
Sheng, Jie;
Shu, Zongmei;
Liang, Jibei] Lanzhou Univ Technol, Sch Life Sci & Engn, Lanzhou 730050, Gansu, Peoples R China;
[Xue, Weiwei;
Yao, Xiaojun] Lanzhou Univ, Dept Chem, Lanzhou 730000, Peoples R China;
[Shi, Yin] CAAS, Key Lab New Anim Drug Project, Key Lab Vet Pharmaceut Dev, Minist Agr,Lanzhou Inst Husb & Pharmaceut Sci, Lanzhou 730050, Gansu, Peoples R China
学科领域Pharmacology & Pharmacy
所属项目编号National Natural Science Foundation of China [21262022] ; Elitist Program of Lanzhou University of Technology [J201303] ; Zhejiang Provincial Natural Science Foundation of China [LY12B02005]
资助项目国家自然科学基金项目
项目资助者National Natural Science Foundation of China [21262022]; Elitist Program of Lanzhou University of Technology [J201303]; Zhejiang Provincial Natural Science Foundation of China [LY12B02005] ; NSFC
DOI10.1007/s00044-013-0905-9
ISSN1054-2523
文章类型Article
语种英语
WOS记录号WOS:000334184400043
第一机构
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文献类型期刊论文
条目标识符http://ir.lzu.edu.cn/handle/262010/81949
Collection化学化工学院
通讯作者Yang, ZD (reprint author), Lanzhou Univ Technol, Sch Life Sci & Engn, Lanzhou 730050, Gansu, Peoples R China.
Recommended Citation:
GB/T 7714
Yang, ZD,Song, ZW,Xue, WW,et al. Synthesis and structure-activity relationship of nuciferine derivatives as potential acetylcholinesterase inhibitors[J]. MEDICINAL CHEMISTRY RESEARCH,2014,23(6).
APA Yang, ZD.,Song, ZW.,Xue, WW.,Sheng, J.,Shu, ZM.,...&Yang, ZD .(2014).Synthesis and structure-activity relationship of nuciferine derivatives as potential acetylcholinesterase inhibitors.MEDICINAL CHEMISTRY RESEARCH,23(6).
MLA Yang, ZD,et al."Synthesis and structure-activity relationship of nuciferine derivatives as potential acetylcholinesterase inhibitors".MEDICINAL CHEMISTRY RESEARCH 23.6(2014).
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