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Triazoloamides as potent γ-secretase modulators with reduced hERG liability. 2012
Christian Fischer, and
Susan L Zultanski, and
Hua Zhou, and
Joey L Methot, and
Sanjiv Shah, and
Hugh Nuthall, and
Bethany L Hughes, and
Nadja Smotrov, and
Armetta Hill, and
Alexander A Szewczak, and
Christopher M Moxham, and
Nathan Bays, and
Richard E Middleton, and
Benito Munoz, and
Mark S Shearman
Merck Research Laboratories Boston, 33 Avenue Louis Pasteur, Boston, MA 02115, USA. christian_fischer@merck.com
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.
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