Substituted 2-oxo-azepane derivatives are potent, orally active γ-secretase inhibitors

A hydroxamic acid screening hit was elaborated to 5,5-difluoro-2-oxoazepane derivatives exhibiting low nanomolar inhibition of γ-secretase, a key proteolytic enzyme involved in Alzheimer’s disease (AD). Oral activity was observed in a transgenic mouse model for AD. A hydroxamic acid screening hit 1...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2008, Vol.18 (1), p.304-308
Hauptverfasser:	Kitas, Eric A., Galley, Guido, Jakob-Roetne, Roland, Flohr, Alexander, Wostl, Wolfgang, Mauser, Harald, Alker, André M., Czech, Christian, Ozmen, Laurence, David-Pierson, Pascale, Reinhardt, Dieter, Jacobsen, Helmut
Format:	Artikel
Sprache:	eng
Schlagworte:	Alzheimer’s disease Amyloid Aβ lowering Amyloid Precursor Protein Secretases - antagonists & inhibitors Animals Azepines - chemical synthesis Azepines - chemistry Azepines - pharmacology Biological and medical sciences Humans Hydroxamic Acids - chemistry In vivo Medical sciences Metabolism Mice Mice, Transgenic Models, Molecular Neuropharmacology Pharmacology. Drug treatments Protease Inhibitors - chemical synthesis Protease Inhibitors - chemistry Protease Inhibitors - pharmacology Proteolytic activity Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease) Psychology. Psychoanalysis. Psychiatry Psychopharmacology Structure-Activity Relationship γ-Secretase
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