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A novel series of potent gamma-secretase inhibitors based on a benzobicyclo[4.2.1]nonane core.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2005 Jan 17; Vol. 15 (2), pp. 373-8. - Publication Year :
- 2005
-
Abstract
- A new series of gamma-secretase inhibitors was developed from an in-house screening hit based on a benzobicyclo[4.2.1]nonane core. Lead optimisation studies led to the development of a series of potent inhibitors and in vivo efficacy was demonstrated.
- Subjects :
- Alkanes pharmacology
Alzheimer Disease drug therapy
Alzheimer Disease metabolism
Amides chemistry
Amines chemistry
Amyloid Precursor Protein Secretases
Animals
Aspartic Acid Endopeptidases
Brain metabolism
Mice
Protease Inhibitors pharmacology
Structure-Activity Relationship
Alkanes chemical synthesis
Brain drug effects
Endopeptidases metabolism
Heterocyclic Compounds chemistry
Protease Inhibitors chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 0960-894X
- Volume :
- 15
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 15603957
- Full Text :
- https://doi.org/10.1016/j.bmcl.2004.10.062