947250-95-5Relevant articles and documents
Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors
Lindsley, Stacey R.,Moore, Keith P.,Rajapakse, Hemaka A.,Selnick, Harold G.,Young, Mary Beth,Zhu, Hong,Munshi, Sanjeev,Kuo, Lawrence,McGaughey, Georgia B.,Colussi, Dennis,Crouthamel, Ming-Chih,Lai, Ming-Tain,Pietrak, Beth,Price, Eric A.,Sankaranarayanan, Sethu,Simon, Adam J.,Seabrook, Guy R.,Hazuda, Daria J.,Pudvah, Nicole T.,Hochman, Jerome H.,Graham, Samuel L.,Vacca, Joseph P.,Nantermet, Philippe G.
, p. 4057 - 4061 (2008/02/10)
This Letter describes the design and synthesis of tertiary carbinamine macrocyclic inhibitors of the β-secretase (BACE-1) enzyme. These macrocyclic inhibitors, some of which incorporate novel P2 substituents, display a 2- to 100-fold increase in potency r
