Phenylimino-2H-chromen-3-carboxamide derivatives as novel small molecule inhibitors of β-secretase (BACE1)

…, A Madadkar-Sobhani, M Khoshneviszadeh…

Index: Edraki, Najmeh; Firuzi, Omidreza; Foroumadi, Alireza; Miri, Ramin; Madadkar-Sobhani, Armin; Khoshneviszadeh, Mehdi; Shafiee, Abbas Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 8 p. 2396 - 2412

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Citation Number: 19

Abstract

The inhibition of β secretase (BACE1) is potentially important approach to treatment of Alzheimer disease (AD). A novel series of 4-bromophenyl piperazine derivatives coupled to the phenylimino-2H-chromen-3-carboxamide scaffold were investigated as BACE1 inhibitors in this study. Docking study suggested that the phenyl-imino group of the scaffold establishes favorable π–π stacking interaction with side chain of Phe108 of flap pocket. ...

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