Fragment-based drug discovery(FBDD) has been widely applied in the research of aspartyl protease inhibitors. In the present study, we reported our work on 2-aminobenzimidazole as the original fragment, which was predicted to bind with the catalytic aspartyl dyad(Asp228 and Asp32) of β-site amyloid precursor protein cleaving enzyme 1(BACE1). A series of novel 2-aminobenzimidazole derivatives were designed and synthesized. The results from FRET assay revealed that three out of the 12 designed 2-aminobenzimida...
【基金】
National Natural Science Foundation of China(Grant No.21002002/21172012)
【更新日期】
2017-10-19
【分类号】
R914
【正文快照】
1.Introduction
Alzheimer’s disease(AD)is an age-related progressive neurodegenerative brain lesion,giving rise to decline in loss of memory and cognitive functions,accompanied by behavioral baffles like aggression and depression[1].The pathological chan
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