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BACE-1 inhibitors part 1: identification of novel hydroxy ethylamines (HEAs).
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 Feb 01; Vol. 18 (3), pp. 1011-6. Date of Electronic Publication: 2007 Dec 15. - Publication Year :
- 2008
-
Abstract
- Inhibition of the aspartyl protease BACE-1 has the potential to deliver a disease-modifying therapy for Alzheimer's disease. Herein, is described the lead generation effort which resulted, with the support of X-ray crystallography, in the discovery of potent inhibitors based on a hydroxy ethylamine (HEA) transition-state mimetic. These inhibitors were capable of lowering amyloid production in a cell-based assay.
- Subjects :
- Alzheimer Disease drug therapy
Amyloid beta-Protein Precursor antagonists & inhibitors
Crystallography, X-Ray
Ethylamines chemistry
Molecular Structure
Structure-Activity Relationship
Alzheimer Disease metabolism
Aspartic Acid Endopeptidases antagonists & inhibitors
Combinatorial Chemistry Techniques
Ethylamines chemical synthesis
Ethylamines pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 18
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 18171614
- Full Text :
- https://doi.org/10.1016/j.bmcl.2007.12.017