Molecular-modeling based design, synthesis, and activity of substituted piperidines as γ-secretase inhibitors

A new series of γ-secretase inhibitors was designed using a ROCS search to identify likely scaffolds. Alzheimer’s disease (AD) is a debilitating disease widely thought to be associated with the accumulation of beta amyloid (Aβ) in the brain. Inhibition of γ-secretase, one of the enzymes responsible...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2005-04, Vol.15 (7), p.1891-1894
Hauptverfasser:	Gundersen, Eric, Fan, Kristi, Haas, Kimberly, Huryn, Donna, Steven Jacobsen, J., Kreft, Anthony, Martone, Robert, Mayer, Scott, Sonnenberg-Reines, June, Sun, Shaiu-Ching, Zhou, Hua
Format:	Artikel
Sprache:	eng
Schlagworte:	Alzheimer Disease - enzymology Alzheimer’s Amyloid beta-Peptides - antagonists & inhibitors Amyloid Precursor Protein Secretases Animals Biological and medical sciences Brain - drug effects Brain - metabolism Drug Design Endopeptidases - drug effects Endopeptidases - metabolism Medical sciences Models, Molecular Molecular modeling Neuropharmacology Pharmacology. Drug treatments Piperidines Piperidines - chemical synthesis Piperidines - pharmacology Protease Inhibitors - chemical synthesis Protease Inhibitors - pharmacology Protein Binding 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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