| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1374044 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
Abstract
The synthesis and SAR of a series of BACE-1 hydroxyethyl amine inhibitors containing substitutions on a spirocyclobutyl moiety is described. Selectivity against cathepsin D, a related aspartyl protease with potential off target toxicity, and improved microsomal stability is exemplified.
Graphical abstractThe structure–activity relationship of the P1′ region of hydroxyethylamine inhibitors of β-secretase (BACE-1) is described.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Holger Monenschein, Daniel B. Horne, Michael D. Bartberger, Stephen A. Hitchcock, Thomas T. Nguyen, Vinod F. Patel, Lewis D. Pennington, Wenge Zhong,