Cyclic sulfamide gamma-secretase inhibitors.
作者信息
Sparey Tim, Beher Dirk, Best Jonathan, Biba Mirlinda, Castro José L, Clarke Earl, Hannam Joanne, Harrison Timothy, Lewis Huw, Madin Andrew, Shearman Mark, Sohal Bindi, Tsou Nancy, Welch Christopher, Wrigley Jonathan
机构信息
Department of Medicinal Chemistry, Merck Sharp and Dohme Research Laboratories, The Neuroscience Research Centre, Terlings Park, Harlow, Essex CM20 2QR, UK.
出版信息
Bioorg Med Chem Lett. 2005 Oct 1;15(19):4212-6. doi: 10.1016/j.bmcl.2005.06.084.
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.
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