Title of article
Cyclic sulfamide γ-secretase inhibitors
Author/Authors
Tim Sparey، نويسنده , , Dirk Beher، نويسنده , , Jonathan Best، نويسنده , , Mirlinda Biba، نويسنده , , José L. Castro، نويسنده , , Earl Clarke، نويسنده , , Joanne Hannam، نويسنده , , Timothy Harrison، نويسنده , , Huw Lewis، نويسنده , , Andrew Madin، نويسنده , , Mark Shearman، نويسنده , , Bindi Sohal، نويسنده , , Nancy Tsou، نويسنده , , Christopher Welch، نويسنده , , Jonathan Wrigley، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
5
From page
4212
To page
4216
Abstract
A novel series of N-alkyl-substituted cyclic sulfamides were developed from a screening hit. Chemistries were developed which allowed surveys of N-alkyl groups and amines resulting in the identification of N-trifluoroethyl-substituted cyclic sulfamides with good in vitro and in vivo γ-secretase activity. One compound with subnanomolar activity elicited a reduction in brain Aβ40 after oral dosing in APP-YAC mice.
Keywords
Alzheimer’s Disease , Cyclic sulfamide , ?-Secretase inhibitor
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795960
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