| Literature DB >> 19811916 |
Jennifer M Sealy1, Anh P Truong, Luke Tso, Gary D Probst, Jose Aquino, Roy K Hom, Barbara M Jagodzinska, Darren Dressen, David W G Wone, Louis Brogley, Varghese John, Jay S Tung, Michael A Pleiss, John A Tucker, Andrei W Konradi, Michael S Dappen, Gergely Toth, Hu Pan, Lany Ruslim, Jim Miller, Michael P Bova, Sukanto Sinha, Kevin P Quinn, John-Michael Sauer.
Abstract
Using structure-guided design, hydroxyethylamine BACE-1 inhibitors were optimized to nanomolar Abeta 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.Entities:
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Year: 2009 PMID： 19811916 DOI： 10.1016/j.bmcl.2009.09.061
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823