Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1376952 | Bioorganic & Medicinal Chemistry Letters | 2008 | 5 Pages |
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.
Graphical abstractExtensive SAR studies led to the identification of 11, which has been extensively profiled in various in vivo settings.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
U. Iserloh, J. Pan, A.W. Stamford, M.E. Kennedy, Q. Zhang, L. Zhang, E.M. Parker, N.A. McHugh, L. Favreau, C. Strickland, J. Voigt,