期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 21, 页码 6721-6727出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.08.097
关键词
A beta amyloid; Alzheimer's disease; beta-Secretase; BACE-1 inhibition; Hydroxylamine (HEA) isostere
A set of low molecular weight compounds containing a hydroxyethylamine (HEA) core structure with different prime side alkyl substituted 4,5,6,7-tetrahydrobenzazoles and one 4,5,6,7-tetrahydropyridinoazole was synthesized. Striking differences were observed on potencies in the BACE-1 enzymatic and cellular assays depending on the nature of the heteroatoms in the bicyclic ring, from the low active compound 4 to inhibitor 6, displaying BACE-1 IC50 values of 44 nM (enzyme assay) and 65 nM (cell-based assay). (C) 2012 Elsevier Ltd. All rights reserved.
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