Synthesis and SAR of hydroxyethylamine based phenylcarboxyamides as inhibitors of BACE

A series of N-((2 S,3 R)-1-(3,5-difluorophenyl)-3-hydroxy-4-(3-methoxybenzylamino)-butan-2-yl)benzamides has been synthesized as BACE inhibitors. A variety of P2 and P3 substituents has been explored, and these efforts have culminated in the identification of several 1,3,5-trisubstituted phenylcarbo...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2009-05, Vol.19 (10), p.2654-2660
Hauptverfasser:	Wu, Yong-Jin, Zhang, Yunhui, Good, Andrew C., Burton, Catherine R., Toyn, Jeremy H., Albright, Charles F., Macor, John E., Thompson, Lorin A.
Format:	Artikel
Sprache:	eng
Schlagworte:	Alzheimer’s disease Amyloid Precursor Protein Secretases - antagonists & inhibitors Amyloid Precursor Protein Secretases - metabolism BACE inhibitor Benzamides - chemical synthesis Benzamides - chemistry Benzamides - pharmacology Biological and medical sciences Cell Line Humans Medical sciences Neuropharmacology Pharmacology. Drug treatments Phenylcarboxyamides Protease Inhibitors - chemical synthesis Protease Inhibitors - chemistry Protease Inhibitors - pharmacology 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 Transfection
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Zusammenfassung:	A series of N-((2 S,3 R)-1-(3,5-difluorophenyl)-3-hydroxy-4-(3-methoxybenzylamino)-butan-2-yl)benzamides has been synthesized as BACE inhibitors. A variety of P2 and P3 substituents has been explored, and these efforts have culminated in the identification of several 1,3,5-trisubstituted phenylcarboxyamides with potent BACE inhibitory activity. A series of N-((2 S,3 R)-1-(3,5-difluorophenyl)-3-hydroxy-4-(3-methoxybenzylamino)-butan-2-yl)benzamides has been synthesized as BACE inhibitors. A variety of P2 and P3 substituents has been explored, and these efforts have culminated in the identification of several 1,3,5-trisubstituted phenylcarboxyamides with potent BACE inhibitory activity.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2009.03.144