Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 24, Issue 11, Pages 2477-2480Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.04.012
Keywords
BACE1 inhibitors; Structure-based ligand design; Alzheimer's disease
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The development of 1,3,4,4a,5,10a-hexahydropyrano[3,4-b]chromene analogs as BACE1 inhibitors is described. Introduction of the spirocyclic pyranochromene scaffold yielded several advantages over previous generation cores, including increased potency, reduced efflux, and reduced CYP2D6 inhibition. Compound 13 ( BACE1 IC50 = 110 nM) demonstrated a reduction in CSF Ab in wild type rats after a single dose. (C) 2014 Elsevier Ltd. All rights reserved.
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