期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 15, 期 19, 页码 4212-4216出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2005.06.084
关键词
Alzheimer's disease; gamma-secretase inhibitor; cyclic sulfamide
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 A beta 40 after oral dosing in APP-YAC mice. (c) 2005 Elsevier Ltd. All rights reserved.
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