期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 3, 页码 1011-1016出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.12.017
关键词
Alzheimer; BACE-1; aspartic protease; hydroxy ethylamine
Inhibition of the aspartyl protease BACE-1 has the potential to deliver a disease-modifying therapy for Alzheimer's disease. Herein, is described the lead generation effort which resulted, with the support of X-ray crystallography, in the discovery of potent inhibitors based on a hydroxy ethylamine (HEA) transition-state mimetic. These inhibitors were capable of lowering amyloid production in a cell-based assay. (C) 2007 Elsevier Ltd. All rights reserved.
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