期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 17, 期 1, 页码 57-62出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.09.094
关键词
gamma-secretase; Alzheimer's disease; inhibitor; sulfonamide; piperidine; carbamate; Mosher ester
A novel piperidine series of gamma-secretase inhibitors, potentially useful for the treatment of Alzheimer's disease, is disclosed. SAR investigation revealed the requirement for cis-stereochemistry of the substituents attached to the core, which resulted in the chair-like diaxial conformation of the piperidine ring. The series was optimized to provide inhibitors with IC(50)'s in the single-digit nanomolar range. Absolute stereochemistry of the active enantiomer was assigned. (c) 2006 Elsevier Ltd. All rights reserved.
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