Bioorganic and Medicinal Chemistry Letters p. 3140 - 3146 (2012)
Update date:2022-08-03
Topics:
Fischer, Christian
Zultanski, Susan L.
Zhou, Hua
Methot, Joey L.
Shah, Sanjiv
Nuthall, Hugh
Hughes, Bethany L.
Smotrov, Nadja
Hill, Armetta
Szewczak, Alexander A.
Moxham, Christopher M.
Bays, Nathan
Middleton, Richard E.
Munoz, Benito
Shearman, Mark S.
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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Doi:10.1007/s00044-012-0069-z
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(2012)Doi:10.1039/c39900000727
(1990)Doi:10.1016/j.molstruc.2012.02.012
(2012)Doi:10.1038/ja.2011.134
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(1991)
