| Literature DB >> 21616665 |
Christian Fischer1, Susan L Zultanski, Hua Zhou, Joey L Methot, W Colby Brown, Dawn M Mampreian, Adam J Schell, Sanjiv Shah, Hugh Nuthall, Bethany L Hughes, Nadja Smotrov, Candia M Kenific, Jonathan C Cruz, Deborah Walker, Melanie Bouthillette, George N Nikov, Dan F Savage, Valentina V Jeliazkova-Mecheva, Damaris Diaz, Alexander A Szewczak, Nathan Bays, Richard E Middleton, Benito Munoz, Mark S Shearman.
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 pharmacokinetics and good central lowering of Aβ42 in Sprague-Dawley rats.Entities:
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Year: 2011 PMID： 21616665 DOI： 10.1016/j.bmcl.2011.04.089
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823