Diamide amino-imidazoles: A novel series of γ-secretase inhibitors for the treatment of Alzheimer’s disease

The synthesis and structure–activity relationship (SAR) of a novel series of di-substituted imidazoles, derived from modification of DAPT, are described. Subsequent optimization led to identification of a highly potent series of inhibitors that contain a β-amine in the imidazole side-chain resulting...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2011-05, Vol.21 (9), p.2631-2636
Hauptverfasser:	Brodney, Michael A., Auperin, David D., Becker, Stacey L., Bronk, Brian S., Brown, Tracy M., Coffman, Karen J., Finley, James E., Hicks, Carol D., Karmilowicz, Michael J., Lanz, Thomas A., Liston, Dane, Liu, Xingrong, Martin, Barbara-Anne, Nelson, Robert B., Nolan, Charles E., Oborski, Christine E., Parker, Christine P., Richter, Karl E.G., Pozdnyakov, Nikolay, Sahagan, Barbara G., Schachter, Joel B., Sokolowski, Sharon A., Tate, Barbara, Van Deusen, Jeffrey W., Wood, Douglas E., Wood, Kathleen M.
Format:	Artikel
Sprache:	eng
Schlagworte:	Alzheimer Disease Amination - drug effects Amino-imidazoles Amyloid beta-Peptides - blood Amyloid beta-Peptides - metabolism Amyloid Precursor Protein Secretases - antagonists & inhibitors Animals Aβ reduction B-lymphocytes Biological and medical sciences Biological Assay brain Diamide - chemical synthesis Diamide - chemistry Diamide - pharmacology Enzyme Activation - drug effects Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Guinea Pigs HeLa Cells Humans imidazoles Imidazoles - chemical synthesis Imidazoles - chemistry Imidazoles - pharmacology Inhibitory Concentration 50 Medical sciences Molecular Structure 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 structure-activity relationships γ-Secretase inhibitors
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