Title of article
Discovery of an orally efficaceous 4-phenoxypyrrolidine-based BACE-1 inhibitor
Author/Authors
U. Iserloh، نويسنده , , J. Pan، نويسنده , , A.W. Stamford، نويسنده , , M.E. Kennedy، نويسنده , , Q. Zhang، نويسنده , , L. Zhang، نويسنده , , E.M. Parker، نويسنده , , N.A. McHugh، نويسنده , , L. Favreau، نويسنده , , C. Strickland، نويسنده , , J. Voigt، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
5
From page
418
To page
422
Abstract
Based on a lead compound identified from the patent literature, we developed patentably novel BACE-1 inhibitors by introducing a cyclic amine scaffold as embodied by 1a and 1b. Extensive SAR studies assessed a variety of isophthalamide replacements including substituted pyrrolidinones and ultimately led to the identification of 11. Due to its favorable overall profile, 11 has been extensively profiled in various in vivo settings.
Keywords
Aspartyl proteases , ?-Secretase inhibitors , Alzheimer’s Disease
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798990
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