874198-93-3Relevant academic research and scientific papers
Design and synthesis of cell potent BACE-1 inhibitors: Structure-activity relationship of P1′ substituents
Sealy, Jennifer M.,Truong, Anh P.,Tso, Luke,Probst, Gary D.,Aquino, Jose,Hom, Roy K.,Jagodzinska, Barbara M.,Dressen, Darren,Wone, David W.G.,Brogley, Louis,John, Varghese,Tung, Jay S.,Pleiss, Michael A.,Tucker, John A.,Konradi, Andrei W.,Dappen, Michael S.,Toth, Gergely,Pan, Hu,Ruslim, Lany,Miller, Jim,Bova, Michael P.,Sinha, Sukanto,Quinn, Kevin P.,Sauer, John-Michael
scheme or table, p. 6386 - 6391 (2010/06/11)
Using structure-guided design, hydroxyethylamine BACE-1 inhibitors were optimized to nanomolar Aβ cellular inhibition with selectivity against cathepsin-D. X-ray crystallography illuminated the S1′ residues critical to this effort, which culminated in compounds 56 and 57 that exhibited potency and selectivity but poor permeability and high P-gp efflux.
OXIME DERIVATIVE SUBSTITUTED HYDROXYETHYLAMINE ASPARTYL PROTEASE INHIBITORS
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Page/Page column 118-119, (2008/06/13)
The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a colletion of diseases, disorders, and conditions associated with abnormal deposition of A-beta protei
OXIME DERIVATIVE HYDROXYETHYLAMINE ASPARTYL-PROTEASE INHIBITORS
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Page/Page column 97-98; 125, (2010/02/15)
The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.
