| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1376911 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
Abstract
The design of amide and heteroaryl amide isosteres as replacements for the carbamate substructure in previously disclosed 2,6-disubstituted piperidine N-arylsulfonamides is described. In several cases, amides lessened CYP liabilities in this class of γ-secretase inhibitors. Selected compounds showed significant reduction of Aβ levels upon oral dosing in a transgenic murine model of Alzheimer’s disease.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Mark D. McBriar, John W. Clader, Inhou Chu, Robert A. Del Vecchio, Leonard Favreau, William J. Greenlee, Lynn A. Hyde, Amin A. Nomeir, Eric M. Parker, Dmitri A. Pissarnitski, Lixin Song, Lili Zhang, Zhiqiang Zhao,