Title of article
Small conformationally restricted piperidine N-arylsulfonamides as orally active γ-secretase inhibitors
Author/Authors
Hubert Josien، نويسنده , , Thomas Bara، نويسنده , , Murali Rajagopalan، نويسنده , , Theodros Asberom، نويسنده , , John W. Clader، 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 , , Gwendolyn T. Wong، نويسنده , , Lili Zhang، نويسنده , , Qi Zhang، نويسنده , , Zhiqiang Zhao، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
6
From page
5330
To page
5335
Abstract
The design and development of a new class of small 2,6-disubstituted piperidine N-arylsulfonamide γ-secretase inhibitors is reported. Lowering molecular weight including the use of conformational constraint led to compounds with less CYP 3A4 liability compared to early leads. Compounds active orally in lowering Aβ levels in Tg CRND8 mice were identified as potential treatments for Alzheimer’s disease.
Keywords
Sulfonamide , piperidine , CYP 3A4 , conformational constraint , inhibitor , Alzheimer’s Disease , ?-Secretase
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798607
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