期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 9, 页码 3140-3146出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.03.054
关键词
Gamma secretase modulator; Alzheimer's; Amyloid beta
Synthesis and SAR studies of novel aryl triazoles as gamma secretase modulators (GSMs) are presented in this communication. Starting from our aryl triazole leads, optimization studies were continued and the series progressed towards novel amides and lactams. Triazole 57 was identified as the most potent analog in this series, displaying single-digit nanomolar A beta 42 IC50 in cell-based assays and reduced affinity for the hERG channel. (C) 2012 Elsevier Ltd. All rights reserved.
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