946420-68-4Relevant articles and documents
Discovery of isonicotinamide derived β-secretase inhibitors: In vivo reduction of β-amyloid
Stanton, Matthew G.,Stauffer, Shaun R.,Gregro, Alison R.,Steinbeiser, Melissa,Nantermet, Philippe,Sankaranarayanan, Sethu,Price, Eric A.,Wu, Guoxin,Crouthamel, Ming-Chih,Ellis, Joan,Lai, Ming-Tain,Espeseth, Amy S.,Shi, Xiao-Ping,Jin, Lixia,Colussi, Dennis,Pietrak, Beth,Huang, Qian,Xu, Min,Simon, Adam J.,Graham, Samuel L.,Vacca, Joseph P.,Selnick, Harold
, p. 3431 - 3433 (2008/02/11)
β-Secretase inhibition offers an exciting opportunity for therapeutic intervention in the progression of Alzheimer's disease. A series of isonicotinamides derived from traditional aspartyl protease transition state isostere inhibitors has been optimized to yield low nanomolar inhibitors with sufficient penetration across the blood-brain barrier to demonstrate β-amyloid lowering in a murine model.