Design and synthesis of thiophene dihydroisoquinolines as novel BACE1 inhibitors

…, P Beroza, H Pan, E Brecht, N Yao, J Lougheed…

Index: Xu, Ying-Zi; Yuan, Shendong; Bowers, Simeon; Hom, Roy K.; Chan, Wayman; Sham, Hing L.; Zhu, Yong L.; Beroza, Paul; Pan, Hu; Brecht, Eric; Yao, Nanhua; Lougheed, Julie; Yan, Jiangli; Tam, Danny; Ren, Zhao; Ruslim, Lany; Bova, Michael P.; Artis, Dean R. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 10 p. 3075 - 3080

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Citation Number: 8

Abstract

Utilizing a structure based design approach, combined with extensive medicinal chemistry execution, highly selective, potent and novel BACE1 inhibitor 8 (BACE1 Alpha assay IC50= 8nM) was made from a weak μM potency hit in an extremely efficient way. The detailed SAR and general design approaches will be discussed.