期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 22, 页码 6386-6391出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.09.061
关键词
Alzheimer's disease; beta-Secretase (BACE-1) inhibitor; Hydroxyethylamine (HEA)
Using structure-guided design, hydroxyethylamine BACE-1 inhibitors were optimized to nanomolar A beta cellular inhibition with selectivity against cathepsin-D. X-ray crystallography illuminated the S1' residues critical to this effort, which culminated in compounds 56 and 57 that exhibited potency and selectivity but poor permeability and high P-gp efflux. (C) 2009 Elsevier Ltd. All rights reserved.
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