期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 3, 页码 844-849出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.11.047
关键词
Alzheimer's disease; gamma-Secretase inhibitor; Structure activity relationship; Sulfone
An investigation is detailed of the structure activity relationships (SAR) of two sulfone side chains of compound (-)-1a (SCH 900229), a potent, PS1-selective gamma-secretase inhibitor and clinical candidate for the treatment of Alzheimer's disease. Specifically, 4-CF3 and 4-Br substituted arylsulfone analogs, (-)-1b and (-)-1c, are equipotent to compound (-)-1a. On the right hand side chain, linker size and terminal substituents of the pendant sulfone group are also investigated. (c) 2012 Elsevier Ltd. All rights reserved.
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