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Structure guided P1' modifications of HEA derived β-secretase inhibitors for the treatment of Alzheimer's disease.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2012 Jun 01; Vol. 22 (11), pp. 3607-11. Date of Electronic Publication: 2012 Apr 19. - Publication Year :
- 2012
-
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.<br /> (Copyright © 2012 Elsevier Ltd. All rights reserved.)
- Subjects :
- Alzheimer Disease drug therapy
Alzheimer Disease metabolism
Alzheimer Disease pathology
Amyloid Precursor Protein Secretases metabolism
Binding Sites
Catalytic Domain
Cathepsin D antagonists & inhibitors
Cathepsin D metabolism
Computer Simulation
Ethylamines chemical synthesis
Ethylamines therapeutic use
Humans
Microsomes, Liver metabolism
Protease Inhibitors chemical synthesis
Protease Inhibitors therapeutic use
Structure-Activity Relationship
Amyloid Precursor Protein Secretases antagonists & inhibitors
Ethylamines chemistry
Protease Inhibitors chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 22
- Issue :
- 11
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 22572583
- Full Text :
- https://doi.org/10.1016/j.bmcl.2012.04.060