Synthesis and SAR study of tricyclic sulfones as γ-secretase inhibitors: C-6 and C-8 positions

SAR exploration at C-6 and C-8 positions of the tricyclic sulfone series was carried out. Several functional groups were found to be well tolerated at C-6 and C-8 positions. Selective combination of C-6 and C-8 modification resulted in new tricyclic sulfone analogs with efficacy in in vivo mouse Aβ...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2011-06, Vol.21 (11), p.3447-3451
Hauptverfasser:	Su, Jing, Tang, Haiqun, McKittrick, Brian A., Xu, Ruo, Clader, John W., Greenlee, William J., Hyde, Lynn, Zhang, Lili
Format:	Artikel
Sprache:	eng
Schlagworte:	Alzheimer’s disease Amyloid beta-Peptides - metabolism Amyloid Precursor Protein Secretases - antagonists & inhibitors Animals Biological and medical sciences chemistry Cyclization Disease Models, Animal Enzyme Activation - drug effects Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Inhibitory Concentration 50 Medical sciences Mice Molecular Structure Neuropharmacology Peptide Fragments - metabolism Pharmacology. Drug treatments 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 Sulfones - chemical synthesis Sulfones - chemistry Sulfones - pharmacology Tricyclic sulfones γ-Secretase inhibitor
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Zusammenfassung:	SAR exploration at C-6 and C-8 positions of the tricyclic sulfone series was carried out. Several functional groups were found to be well tolerated at C-6 and C-8 positions. Selective combination of C-6 and C-8 modification resulted in new tricyclic sulfone analogs with efficacy in in vivo mouse Aβ 40 lowering model.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2011.03.094