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 ,
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.
