A new series of potent benzodiazepine γ-secretase inhibitors

A new series of benzodiazepine-containing γ-secretase inhibitors with potential use in the treatment of Alzheimer's disease is disclosed. Structure–activity relationships of the pendant hydrocinnamate side-chain which led to the preparation of highly potent inhibitors are described. The structu...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2003-01, Vol.13 (2), p.179-183
Main Authors: Churcher, Ian, Ashton, Kate, Butcher, John W., Clarke, Earl E., Harrison, Timothy, Lewis, Huw D., Owens, Andrew P., Teall, Martin R., Williams, Susie, Wrigley, Jonathan D.J.
Format: Article
Language:English
Subjects:
Amyloid Precursor Protein Secretases
Aspartic Acid Endopeptidases
Benzodiazepines - chemical synthesis
Benzodiazepines - pharmacology
Biological and medical sciences
Cell Line
Endopeptidases - metabolism
Humans
Indicators and Reagents
Medical sciences
Molecular Conformation
Neuropharmacology
Pharmacology. Drug treatments
Protease Inhibitors - chemical synthesis
Protease Inhibitors - pharmacology
Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease)
Psychology. Psychoanalysis. Psychiatry
Psychopharmacology
Structure-Activity Relationship
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Summary:A new series of benzodiazepine-containing γ-secretase inhibitors with potential use in the treatment of Alzheimer's disease is disclosed. Structure–activity relationships of the pendant hydrocinnamate side-chain which led to the preparation of highly potent inhibitors are described. The structure–activity relationships of a series of γ-secretase inhibitors are discussed.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(02)00909-5