| Literature DB >> 16054361 |
Tim Sparey1, Dirk Beher, Jonathan Best, Mirlinda Biba, José L Castro, Earl Clarke, Joanne Hannam, Timothy Harrison, Huw Lewis, Andrew Madin, Mark Shearman, Bindi Sohal, Nancy Tsou, Christopher Welch, Jonathan Wrigley.
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 gamma-secretase activity. One compound with subnanomolar activity elicited a reduction in brain Abeta40 after oral dosing in APP-YAC mice.Entities:
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Year: 2005 PMID： 16054361 DOI： 10.1016/j.bmcl.2005.06.084
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823