1. |
- Sandgren, Veronica, et al.
(author)
-
Design and synthesis of hydroxyethylene-based BACE-1 inhibitors incorporating extended P1 substituents
- 2013
-
In: Open Medicinal Chemistry Journal. - Bussum, Netherlands : Bentham Open. - 1874-1045. ; 7, s. 1-15
-
Journal article (peer-reviewed)abstract
- Novel BACE-1 inhibitors with a hydroxyethylene central core have been developed. Modified P1´ and extended P1 substituents were incorporated with the aim to explore potential interactions with the S1´ and the S1-S3 pocket, respectively, of BACE-1. Inhibitors were identified displaying IC50 values in the nanomolar range, i.e., 69 nM for the most potent compound. Possible inhibitor interactions with the enzyme are also discussed.
|
|