| Literature DB >> 22497762 |
Christian Fischer1, 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.
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 IC(50) in cell-based assays and reduced affinity for the hERG channel.Entities:
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Year: 2012 PMID： 22497762 DOI： 10.1016/j.bmcl.2012.03.054
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823