| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10592477 | Bioorganic & Medicinal Chemistry Letters | 2012 | 7 Pages |
Abstract
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 Aβ42 IC50 in cell-based assays and reduced affinity for the hERG channel.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Christian Fischer, Susan L. Zultanski, Hua Zhou, Joey L. Methot, Sanjiv Shah, Hugh Nuthall, Bethany L. Hughes, Nadja Smotrov, Armetta Hill, Alexander A. Szewczak, Christopher M. Moxham, Nathan Bays, Richard E. Middleton, Benito Munoz, Mark S. Shearman,