Title of article
Discovery of amide and heteroaryl isosteres as carbamate replacements in a series of orally active γ-secretase inhibitors
Author/Authors
Mark D. McBriar، نويسنده , , John W. Clader، نويسنده , , Inhou Chu، نويسنده , , Robert A. Del Vecchio، نويسنده , , Leonard Favreau، نويسنده , , William J. Greenlee، نويسنده , , Lynn A. Hyde، نويسنده , , Amin A. Nomeir، نويسنده , , Eric M. Parker، نويسنده , , Dmitri A. Pissarnitski، نويسنده , , Lixin Song، نويسنده , , Lili Zhang، نويسنده , , Zhiqiang Zhao، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
5
From page
215
To page
219
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.
Keywords
Alzheimer’s disease , ?-Secretase
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798949
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