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

Authors :
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
Source :
Bioorganic & Medicinal Chemistry Letters. Oct2010, Vol. 20 Issue 20, p6034-6039. 6p.
Publication Year :
2010

Abstract

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. [Copyright &y& Elsevier]

Details

Language :
English
ISSN :
0960894X
Volume :
20
Issue :
20
Database :
Academic Search Index
Journal :
Bioorganic & Medicinal Chemistry Letters
Publication Type :
Academic Journal
Accession number :
53789732
Full Text :
https://doi.org/10.1016/j.bmcl.2010.08.070