期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 11, 页码 2477-2480出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.04.012
关键词
BACE1 inhibitors; Structure-based ligand design; Alzheimer's disease
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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