Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 11, Pages 3607-3611Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.04.060
Keywords
A beta amyloid; Alzheimer's disease; Aspartyl protease; beta-secretase; BACE inhibitors; Hydroxyethylene derivatives; Protease inhibitors
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The synthesis and SAR of a series of BACE-1 hydroxyethyl amine inhibitors containing substitutions on a spirocyclobutyl moiety is described. Selectivity against cathepsin D, a related aspartyl protease with potential off target toxicity, and improved microsomal stability is exemplified. (C) 2012 Elsevier Ltd. All rights reserved.
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