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Synthesis and preliminary evaluation of peptidomimetic inhibitors of human beta-secretase
Niu, Yan1; Wang, Yuehua2; Zou, Xiaomin1; Yang, Xiaoming1; Ma, Chao1; Lue, Yang1; Zhou, Bo1; Yuan, Yue1; Du, Guanhua2; Xu, Ping1
关键词Beta-secretase Inhibitor Hydroxyethylene Isostere Cadd Peptidomimetic Synthesis
刊名EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
2010-05-01
DOI10.1016/j.ejmech.2010.01.044
45期:5页:2089-2094
收录类别SCI ; IC
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Medicinal
资助者National Natural Science Foundation of China ; National Natural Science Foundation of China
研究领域[WOS]Pharmacology & Pharmacy
关键词[WOS]ALZHEIMERS-DISEASE ; POTENT INHIBITORS ; PROTEASE ; DESIGN ; BACE
英文摘要

Based on the structure of OM99-2 and the X-ray crystal structure of its complex with beta-secretase, a series of compounds containing the Leu*Ala hydroxyethylene isostere as a scissile bond substitution were designed. 31 compounds were synthesized and their beta-secretase inhibition activities were measured. It was found that isobutyl group was a better R(3) substitution as C-terminus in our target compounds, and 4-nitrobenzyl group was the best R(2) side chain. With the aid of molecular modeling, the binding modes of compounds 9 and 22 with beta-secretase were compared. The result revealed a stronger bonding mode of 22 than 9. This explored that the optimal length of this series of peptidomimetic inhibitors was P3-P2′. The molecular weights of compounds with this length are around 600. (C) 2010 Elsevier Masson SAS. All rights reserved.

语种英语
所属项目编号30772650 ; 20772008
资助者National Natural Science Foundation of China ; National Natural Science Foundation of China
WOS记录号WOS:000276695200051
引用统计
被引频次:2[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/52030
专题北京大学药学院_药物化学系
作者单位1.Peking Univ, Sch Pharmaceut Sci, Dept Med Chem, Beijing 100191, Peoples R China
2.Chinese Acad Med Sci, Inst Mat Med, Beijing 100050, Peoples R China
推荐引用方式
GB/T 7714
Niu, Yan,Wang, Yuehua,Zou, Xiaomin,et al. Synthesis and preliminary evaluation of peptidomimetic inhibitors of human beta-secretase[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2010,45(5):2089-2094.
APA Niu, Yan.,Wang, Yuehua.,Zou, Xiaomin.,Yang, Xiaoming.,Ma, Chao.,...&Xu, Ping.(2010).Synthesis and preliminary evaluation of peptidomimetic inhibitors of human beta-secretase.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,45(5),2089-2094.
MLA Niu, Yan,et al."Synthesis and preliminary evaluation of peptidomimetic inhibitors of human beta-secretase".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 45.5(2010):2089-2094.
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