423168-79-0Relevant articles and documents
Cyclic sulfamide γ-secretase inhibitors
Sparey, Tim,Beher, Dirk,Best, Jonathan,Biba, Mirlinda,Castro, Jose L.,Clarke, Earl,Hannam, Joanne,Harrison, Timothy,Lewis, Huw,Madin, Andrew,Shearman, Mark,Sohal, Bindi,Tsou, Nancy,Welch, Christopher,Wrigley, Jonathan
, p. 4212 - 4216 (2007/10/03)
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.
