Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10593002 | Bioorganic & Medicinal Chemistry Letters | 2013 | 7 Pages |
Abstract
Previous structure based optimization in our laboratories led to the identification of a novel, high-affinity cyclic sulfone hydroxyethylamine-derived inhibitor such as 1 that lowers CNS-derived Aβ following oral administration to transgenic APP51/16 mice. Herein we report SAR development in the S3 and S2Ⲡsubsites of BACE1 for cyclic sulfoxide hydroxyethyl amine inhibitors, the synthetic approaches employed in this effort, and in vivo data for optimized compound such as 11d.
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Authors
Heinrich Rueeger, Rainer Lueoend, Rainer Machauer, Siem Jacob Veenstra, Laura Helen Jacobson, Matthias Staufenbiel, Sandrine Desrayaud, Jean-Michel Rondeau, Henrik Möbitz, Ulf Neumann,