928330-65-8Relevant articles and documents
Discovery of oxadiazoyl tertiary carbinamine inhibitors of β-secretase (BACE-1)
Rajapakse, Hemaka A.,Nantermet, Philippe G.,Selnick, Harold G.,Munshi, Sanjeev,McGaughey, Georgia B.,Lindsley, Stacey R.,Young, Mary Beth,Lai, Ming-Tain,Espeseth, Amy S.,Shi, Xiao-Ping,Colussi, Dennis,Pietrak, Beth,Crouthamel, Ming-Chih,Tugusheva, Katherine,Huang, Qian,Xu, Min,Simon, Adam J.,Kuo, Lawrence,Hazuda, Daria J.,Graham, Samuel,Vacca, Joseph P.
, p. 7270 - 7273 (2007/10/03)
We describe the discovery and optimization of tertiary carbinamine derived inhibitors of the enzyme β-secretase (BACE-1). These novel non-transition-state-derived ligands incorporate a single primary amine to interact with the catalytic aspartates of the