3,4-Fused cyclohexyl sulfones as γ-secretase inhibitors

The identification of a potent γ-secretase inhibitor, for example (ED 50 = 0.06 nM), is reported. The 3,4-fused sulfamides, sulfonamides and sulfone have been identified as highly potent γ-secretase inhibitors. Evaluation of the SAR of substitution within these series has allowed the identification...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2006-06, Vol.16 (11), p.3073-3077
Hauptverfasser:	Shaw, Duncan, Best, Jonathan, Dinnell, Kevin, Nadin, Alan, Shearman, Mark, Pattison, Christine, Peachey, James, Reilly, Michael, Williams, Brian, Wrigley, Jonathan, Harrison, Timothy
Format:	Artikel
Sprache:	eng
Schlagworte:	Alzheimer’s disease Amyloid Precursor Protein Secretases Animals Aspartic Acid Endopeptidases Biological and medical sciences Crystallography, X-Ray Cyclization Endopeptidases - metabolism Medical sciences Models, Molecular Molecular Structure Neuropharmacology Pharmacology. Drug treatments Protease Inhibitors - chemical synthesis Protease Inhibitors - chemistry Protease Inhibitors - pharmacology Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease) Psychology. Psychoanalysis. Psychiatry Psychopharmacology Rats Structure-Activity Relationship Sulfones Sulfones - chemical synthesis Sulfones - chemistry Sulfones - pharmacology γ-Secretase inhibitors
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