Design, synthesis, and structure–activity relationship studies of N-arylsulfonyl morpholines as γ-secretase inhibitors

Design and synthesis of cis-2,6-disubstituted N-arylsulfonyl morpholines as novel γ-secretase inhibitors for the potential treatment of Alzheimer’s disease (AD) is reported. Several different small alkyl groups are installed on the left-hand side to lower the CYP3A4 liability while maintaining excel...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-11, Vol.20 (22), p.6606-6609
Hauptverfasser:	Li, Hongmei, Xu, Ruo, Cole, David, Clader, John W., Greenlee, William J., Nomeir, Amin A., Song, Lixin, Zhang, Lili
Format:	Artikel
Sprache:	eng
Schlagworte:	Alzheimer’s disease Amyloid Precursor Protein Secretases - antagonists & inhibitors Biological and medical sciences Drug Design Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Medical sciences Morpholines - chemical synthesis Morpholines - chemistry Morpholines - pharmacology Neuropharmacology 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 γ-Secretase inhibitors
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Beschreibung
Zusammenfassung:	Design and synthesis of cis-2,6-disubstituted N-arylsulfonyl morpholines as novel γ-secretase inhibitors for the potential treatment of Alzheimer’s disease (AD) is reported. Several different small alkyl groups are installed on the left-hand side to lower the CYP3A4 liability while maintaining excellent in vitro potency.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2010.09.028