1428732-40-4Relevant articles and documents
Structure-based design of novel dihydroisoquinoline BACE-1 inhibitors that do not engage the catalytic aspartates
Bowers, Simeon,Xu, Ying-Zi,Yuan, Shendong,Probst, Gary D.,Hom, Roy K.,Chan, Wayman,Konradi, Andrei W.,Sham, Hing L.,Zhu, Yong L.,Beroza, Paul,Pan, Hu,Brecht, Eric,Yao, Nanhua,Lougheed, Julie,Tam, Danny,Ren, Zhao,Ruslim, Lany,Bova, Michael P.,Artis, Dean R.
, p. 2181 - 2186 (2013/04/23)
The structure-activity relationship of a series of dihydroisoquinoline BACE-1 inhibitors is described. Application of structure-based design to screening hit 1 yielded sub-micromolar inhibitors. Replacement of the carboxylic acid of 1 was guided by X-ray
