期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 7, 页码 2181-2186出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.01.103
关键词
Alzheimer's disease; Beta-secretase; BACE-1 inhibitor
The structure-activity relationship of a series of dihydroisoquinoline BACE-1 inhibitors is described. Application of structure-based design to screening hit 1 yielded sub-micromolar inhibitors. Replacement of the carboxylic acid of 1 was guided by X-ray crystallography, which allowed the replacement of a key water-mediated hydrogen bond. This work culminated in compounds such as 31, which possess good BACE-1 potency, excellent permeability and a low P-gp efflux ratio. (C) 2013 Elsevier Ltd. All rights reserved.
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