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用于治疗阿尔茨海默病的基于3-取代偕二环己烷砜的γ-分泌酶抑制剂:构象分析与生物活性

3-Substituted gem-cyclohexane sulfone based gamma-secretase inhibitors for Alzheimer's disease: conformational analysis and biological activity.

作者信息

Jelley Richard A, Elliott Jason, Gibson Karl R, Harrison Timothy, Beher Dirk, Clarke Earl E, Lewis Huw D, Shearman Mark, Wrigley Jonathan D J

机构信息

Department of Medicinal Chemistry, Merck Sharp and Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Eastwick Road, Harlow, Essex CM20 2QR, UK.

出版信息

Bioorg Med Chem Lett. 2006 Jul 15;16(14):3839-42. doi: 10.1016/j.bmcl.2006.04.019. Epub 2006 May 6.

Abstract

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.

摘要

此前,针对γ-分泌酶抑制剂的宝石型环己烷系列的化学研究工作主要集中在环己烷环的4位。最近,化学研究方向转向了3位,在此处进行取代也得到了具有高γ-分泌酶活性的化合物。

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