935460-12-1Relevant articles and documents
Improving the permeability of the hydroxyethylamine BACE-1 inhibitors: Structure-activity relationship of P2′ substituents
Truong, Anh P.,Probst, Gary D.,Aquino, Jose,Fang, Larry,Brogley, Louis,Sealy, Jennifer M.,Hom, Roy K.,Tucker, John A.,John, Varghese,Tung, Jay S.,Pleiss, Michael A.,Konradi, Andrei W.,Sham, Hing L.,Dappen, Michael S.,Toth, Gergley,Yao, Nanhua,Brecht, Eric,Pan, Hu,Artis, Dean R.,Ruslim, Lany,Bova, Michael P.,Sinha, Sukanto,Yednock, Ted A.,Zmolek, Wes,Quinn, Kevin P.,Sauer, John-Michael
scheme or table, p. 4789 - 4794 (2010/11/02)
Herein we describe further evolution of hydroxyethylamine inhibitors of BACE-1 with enhanced permeability characteristics necessary for CNS penetration. Variation at the P2′ position of the inhibitor with more polar substituents led to compounds 19 and 32