3-Substituted gem-cyclohexane sulfone based γ-secretase inhibitors for Alzheimer's disease:: Conformational analysis and biological activity

被引：17

作者：

Jelley, Richard A.

Elliott, Jason

Gibson, Karl R.

Harrison, Timothy

Beher, Dirk

Clarke, Earl E.

Lewis, Huw D.

Shearman, Mark

Wrigley, Jonathan D. J.

机构：

[1] Neurosci Res Ctr, Merck Sharp & Dohme Res Labs, Dept Med Chem, Harlow CM20 2QR, Essex, England

[2] Merck Sharp & Dohme Ltd, Dept Mol & Cellular Neurosci, Ctr Res Neurosci, Harlow CM20 2QR, Essex, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 14期

关键词：

gem-cyclohexane; sulfone; gamma-secretase inhibitors; Alzheimer's disease; conformational analysis; biological activity;

D O I：

10.1016/j.bmcl.2006.04.019

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Previously, chemistry effort on the gem-cyclohexane series of gamma-secretase inhibitors has focused on the 4-position of the cyclohexane ring. Recently chemistry has been directed towards the 3-position and substitution here has also provided compounds with high gamma-secretase activity. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：3839 / 3842

页数：4

共 8 条

[1] Chemoselective cross-metathesis reaction. Application to the synthesis of the C1-C14 fragment of amphidinol 3 [J].