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学科主题: 药学
题名:
Design, Synthesis and In Vitro Biological Evaluation of 3-styrylbenzimidamides as Potential BACE1 Inhibitors
作者: Niu, Yan; Gao, Haifei; Xu, Fengrong; Liang, Lei; Liu, Peng; Wang, Chao; Yang, Guanyu; Sun, Qi; Xu, Ping
关键词: Alzheimer&prime ; s disease ; BACE1 inhibitors ; 3-styrylbenzimidamide ; CADD
刊名: LETTERS IN DRUG DESIGN & DISCOVERY
发表日期: 2013-05-01
卷: 10, 期:4, 页:297-302
收录类别: SCI
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]: ALZHEIMERS-DISEASE
英文摘要:

A series of 3-styrylbenzimidamides were synthesized and biologically evaluated in a cell free FRET assay as potential BACE1 inhibitors. Some of the synthesized analogues were discovered to have moderate BACE1 inhibitory activities with IC50 values ranging from 9.3 to 295.8 mu M. Molecular docking study proposed that the most potent compound (E)-2d bound to BACE1 differently in S3-S2′ subpockets forming no polar interaction with the catalytic Asp dyad compared with the 3-styrylbenzimidamides. The results would contribute to the further optimizations on benzimidamide scaffold to achieve novel small molecular BACE1 inhibitors with improved potencies.

语种: 英语
所属项目编号: 21002002 ; 21172012 ; 2012CB518000
项目资助者: National Natural Science Foundation of China ; National Basic Research Program of China
WOS记录号: WOS:000317927800002
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/67798
Appears in Collections:北京大学药学院_期刊论文

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作者单位: Peking Univ, Hlth Sci Ctr, Sch Pharmaceut Sci, Dept Med Chem,State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China

Recommended Citation:
Niu, Yan,Gao, Haifei,Xu, Fengrong,et al. Design, Synthesis and In Vitro Biological Evaluation of 3-styrylbenzimidamides as Potential BACE1 Inhibitors[J]. LETTERS IN DRUG DESIGN & DISCOVERY,2013,10(4):297-302.
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