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
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- PMID: 20822903
- DOI: 10.1016/j.bmcl.2010.08.070
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Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: structure-activity relationship of the aryl region
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.
Copyright © 2010 Elsevier Ltd. All rights reserved.
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