BACE-1 inhibition by a series of ψ[CH 2NH] reduced amide isosteres

A new class of β-secretase inhibitors that incorporate a reduced amide transition state isostere as the key binding element is described. The incorporation of a 5-substituted isophthalamide scaffold at the N-terminal site of this isostere resulted in potent compounds that display impressive cellular...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2006-07, Vol.16 (14), p.3635-3638
Hauptverfasser:	Coburn, Craig A., Stachel, Shawn J., Jones, Kristen G., Steele, Thomas G., Rush, Diane M., DiMuzio, Jillian, Pietrak, Beth L., Lai, Ming-Tain, Huang, Qian, Lineberger, Janet, Jin, Lixia, Munshi, Sanjeev, Katharine Holloway, M., Espeseth, Amy, Simon, Adam, Hazuda, Daria, Graham, Samuel L., Vacca, Joseph P.
Format:	Artikel
Sprache:	eng
Schlagworte:	Amides - chemistry Amyloid Precursor Protein Secretases Binding Sites Biological and medical sciences Endopeptidases - metabolism Immunoassay Isostere Medical sciences Neuropharmacology Peptides - chemistry Pharmacology. Drug treatments Protease Inhibitors - chemical synthesis Protease Inhibitors - pharmacology Psychoanaleptics: cns stimulant, antidepressant agent, nootropic agent, mood stabilizer..., (alzheimer disease) Psychology. Psychoanalysis. Psychiatry Psychopharmacology Reduced amide Structure-Activity Relationship β-Secretase
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