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4-Oxo-1,4-dihydro-quinoline-3-carboxamides as BACE-1 inhibitors: Synthesis, biological evaluation and docking studies
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
2014-05-22
DOI10.1016/j.ejmech.2014.04.025
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
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 ; National Natural Science Foundation of China ; National Basic Research Program of China ; Specialized Research Fund for the Doctoral Program of Higher Education of China
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
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 ; 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
引用统计
被引频次:7[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/400002259/63646
专题北京大学药学院_药物化学系
作者单位Peking Univ, Hlth Sci Ctr, Sch Pharmaceut Sci, Dept Med Chem, Beijing 100191, Peoples R China
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GB/T 7714
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.
APA Liu, Peng.,Niu, Yan.,Wang, Chao.,Sun, Qi.,Zhai, Yaya.,...&Xu, Ping.(2014).4-Oxo-1,4-dihydro-quinoline-3-carboxamides as BACE-1 inhibitors: Synthesis, biological evaluation and docking studies.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,79,413-421.
MLA Liu, Peng,et al."4-Oxo-1,4-dihydro-quinoline-3-carboxamides as BACE-1 inhibitors: Synthesis, biological evaluation and docking studies".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 79(2014):413-421.
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