Triazoles as γ-secretase modulators

…, H Zhou, JL Methot, WC Brown, DM Mampreian…

Index: Fischer, Christian; Zultanski, Susan L.; Zhou, Hua; Methot, Joey L.; Brown, W. Colby; Mampreian, Dawn M.; Schell, Adam J.; Shah, Sanjiv; Nuthall, Hugh; Hughes, Bethany L.; Smotrov, Nadja; Kenific, Candia M.; Cruz, Jonathan C.; Walker, Deborah; Bouthillette, Melanie; Nikov, George N.; Savage, Dan F.; Jeliazkova-Mecheva, Valentina V.; Diaz, Damaris; Szewczak, Alexander A.; Bays, Nathan; Middleton, Richard E.; Munoz, Benito; Shearman, Mark S. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 13 p. 4083 - 4087

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Citation Number: 18

Abstract

Abstract Synthesis, SAR, and evaluation of aryl triazoles as novel gamma secretase modulators (GSMs) are presented in this communication. Starting from the literature and in- house leads, we evaluated a range of five-membered heterocycles as replacements for olefins commonly found in non-acid GSMs. 1, 2, 3-C-aryl-triazoles were identified as suitable replacements which exhibited good modulation of γ-secretase activity, excellent ...