3,4-Fused cyclohexyl sulfiones as γ-secretase inhibitors

被引:24
|
作者
Shaw, D
Best, J
Dinnell, K
Nadin, A
Shearman, M
Pattison, C
Peachey, J
Reilly, M
Williams, B
Wrigley, J
Harrison, T
机构
[1] Ctr Res Neurosci, Dept Med Chem, Harlow CM20 2QR, Essex, England
[2] Ctr Res Neurosci, Dept Mol & Cellular Neurosci, Harlow CM20 2QR, Essex, England
[3] Ctr Res Neurosci, Dept Vivo Neurosci, Harlow CM20 2QR, Essex, England
关键词
sulfones; gamma-secretase inhibitors; Alzheimer's disease;
D O I
10.1016/j.bmcl.2005.12.083
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The 3,4-fused sulfamides, sulfonamides and sulfone have been identified as highly potent gamma-secretase inhibitors. Evaluation of the SAR of substitution within these series has allowed the identification of a range of compounds which significantly reduce brain A beta in transgenic mouse models and thus have potential as possible treatments for Alzheimer's disease. (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3073 / 3077
页数:5
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