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学科主题: 药学
题名:
4-Oxo-1,4-dihydro-quinoline-3-carboxamides as BACE-1 inhibitors: Synthesis, biological evaluation and docking studies
作者: Liu, Peng; Niu, Yan; Wang, Chao; Sun, Qi; Zhai, Yaya; Yu, Jiapei; Sun, Jing; Xu, Fengrong; Yan, Gang; Huang, Wenjie; Liang, Lei; Xu, Ping
关键词: Alzheimer&prime ; s disease ; BACE-1 inhibitors ; 4-Oxo-1,4-dihydro-quinoline-3-carboxamide ; Docking study
刊名: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
发表日期: 2014-05-22
DOI: 10.1016/j.ejmech.2014.04.025
卷: 79, 页:413-421
收录类别: SCI ; IC
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Chemistry, Medicinal
研究领域[WOS]: Pharmacology & Pharmacy
关键词[WOS]: MEMAPSIN-2 BETA-SECRETASE ; ALZHEIMERS-DISEASE ; ACRIDONE ALKALOIDS ; DESIGN ; OPTIMIZATION ; QUINAZOLINE ; DERIVATIVES ; DISCOVERY ; QUINOLINE
英文摘要:

In this work, we report a series of new 4-oxo-1,4-dihydro-quinoline-3-carboxamide derivatives as,beta-secretase (BACE-1) inhibitors. Supported by docking study, a small library of derivatives were designed, synthesized and biologically evaluated in vitro. The studies revealed that the most potent analog 14e (IC50 = 1.89 mu M) with low cellular cytotoxicity and high predicted blood brain barrier permeability, could serve as a good structure for further modification.(c) 2014 Elsevier Masson SAS. All rights reserved.

语种: 英语
所属项目编号: 21002002 ; 21172012 ; 2012CB518000 ; 20120001110010
项目资助者: National Natural Science Foundation of China ; National Basic Research Program of China ; Specialized Research Fund for the Doctoral Program of Higher Education of China
WOS记录号: WOS:000336700600038
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/63646
Appears in Collections:北京大学药学院_药物化学系_期刊论文

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作者单位: Peking Univ, Hlth Sci Ctr, Sch Pharmaceut Sci, Dept Med Chem, Beijing 100191, Peoples R China

Recommended Citation:
Liu, Peng,Niu, Yan,Wang, Chao,et al. 4-Oxo-1,4-dihydro-quinoline-3-carboxamides as BACE-1 inhibitors: Synthesis, biological evaluation and docking studies[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2014,79:413-421.
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