期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 22, 页码 6909-6915出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.06.116
关键词
BACE-1 inhibitors; Alzheimer's disease; BACE-1 crystallography; P-gp knockout mice
The synthesis, evaluation, and structure-activity relationships of a set of related constrained diaminopropane inhibitors of BACE-1 are described. The full in vivo profile of an optimized inhibitor in both normal and P-gp deficient mice is compared with data generated in normal rats. (C) 2011 Elsevier Ltd. All rights reserved.
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