Molecules

Virtual screening and structure-based discovery of indole acylguanidines as potent β-secretase (BACE1) inhibitors

Y Zou, L Li, W Chen, T Chen, L Ma, X Wang, B Xiong…

Index: Zou, Yiquan; Li, Li; Chen, Wuyan; Chen, Tiantian; Ma, Lanping; Wang, Xin; Xiong, Bing; Xu, Yechun; Shen, Jingkang Molecules, 2013 , vol. 18, # 5 p. 5706 - 5722

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Citation Number: 9

Abstract

Abstract: Proteolytic cleavage of amyloid precursor protein by β-secretase (BACE1) is a key step in generating the N-terminal of β-amyloid (Aβ), which further forms into amyloid plaques that are considered as the hallmark of Alzheimer's disease. Inhibitors of BACE1 can reduce the levels of Aβ and thus have a therapeutic potential for treating the disease. We report here the identification of a series of small molecules bearing an indole acylguanidine core ...