31767-01-8Relevant academic research and scientific papers
Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: Structure-activity relationship of the aryl region
Probst, Gary D.,Bowers, Simeon,Sealy, Jennifer M.,Stupi, Brian,Dressen, Darren,Jagodzinska, Barbara M.,Aquino, Jose,Gailunas, Andrea,Truong, Anh P.,Tso, Luke,Xu, Ying-Zi,Hom, Roy K.,John, Varghese,Tung, Jay S.,Pleiss, Michael A.,Tucker, John A.,Konradi, Andrei W.,Sham, Hing L.,Jagodzinski, Jacek,Toth, Gergely,Brecht, Eric,Yao, Nanhua,Pan, Hu,Lin, May,Artis, Dean R.,Ruslim, Lany,Bova, Michael P.,Sinha, Sukanto,Yednock, Ted A.,Gauby, Shawn,Zmolek, Wes,Quinn, Kevin P.,Sauer, John-Michael
scheme or table, p. 6034 - 6039 (2010/11/04)
The structure-activity relationship of the prime region of hydroxyethylamine BACE inhibitors is described. Variation in the aryl linker region with 5- and 6-membered heterocycles provided compounds such as 33 with improved permeability and reduced P-gp liability compared to benzyl amine analog 1.
Inhibition of IKK-2 by 2-[(aminocarbonyl)amino]-5-acetylenyl-3- thiophenecarboxamides
Bonafoux, Dominique,Bonar, Sheri,Christine, Lori,Clare, Michael,Donnelly, Ann,Guzova, Julia,Kishore, Nandini,Lennon, Patrick,Libby, Adam,Mathialagan, Sumathy,McGhee, William,Rouw, Sharon,Sommers, Cindy,Tollefson, Michael,Tripp, Catherine,Weier, Richard,Wolfson, Serge,Min, Yao
, p. 2870 - 2875 (2007/10/03)
A series of 21 novel 2-[(aminocarbonyl)amino]-5-acetylenyl-3- thiophenecarboxamides were synthesized and evaluated for the inhibition of IKK-2. In spite of their often modest activity on the enzyme, six selected analogs showed significant inhibition of th
