| Literature DB >> 20822903 |
Gary D Probst1, Simeon Bowers, Jennifer M Sealy, Brian Stupi, Darren Dressen, Barbara M Jagodzinska, Jose Aquino, Andrea Gailunas, Anh P Truong, Luke Tso, Ying-Zi Xu, Roy K Hom, Varghese John, Jay S Tung, Michael A Pleiss, John A Tucker, Andrei W Konradi, Hing L Sham, Jacek Jagodzinski, Gergely Toth, Eric Brecht, Nanhua Yao, Hu Pan, May Lin, Dean R Artis, Lany Ruslim, Michael P Bova, Sukanto Sinha, Ted A Yednock, Shawn Gauby, Wes Zmolek, Kevin P Quinn, John-Michael Sauer.
Abstract
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.Entities:
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Year: 2010 PMID： 20822903 DOI： 10.1016/j.bmcl.2010.08.070
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823