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. 2010 Oct 15;20(20):6034-9.
doi: 10.1016/j.bmcl.2010.08.070. Epub 2010 Aug 19.

Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: structure-activity relationship of the aryl region

Gary D Probst  1 , 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
Affiliations

Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: structure-activity relationship of the aryl region

Gary D Probst et al. Bioorg Med Chem Lett. .

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.

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