| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1372964 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
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.
Graphical abstractSynthesis, 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.Figure optionsDownload full-size imageDownload as PowerPoint slide
