Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: Prime side chromane-containing inhibitors

The structure activity relationship of the prime region of conformationally restricted hydroxyethylamine (HEA) BACE inhibitors is described. Variation of the P1′ region provided selectivity over Cat-D with a series of 2,2-dioxo-isothiochromanes and optimization of the P2′ substituent of chromane–HEA...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2013-08, Vol.23 (16), p.4674-4679
Hauptverfasser:	Ng, Raymond A., Sun, Minghua, Bowers, Simeon, Hom, Roy K., Probst, Gary D., John, Varghese, Fang, Lawrence Y., Maillard, Michel, Gailunas, Andrea, Brogley, Louis, Neitz, R. Jeffrey, Tung, Jay S., Pleiss, Michael A., Konradi, Andrei W., Sham, Hing L., Dappen, Michael S., Adler, Marc, Yao, Nanhua, Zmolek, Wes, Nakamura, David, Quinn, Kevin P., Sauer, John-Michael, Bova, Michael P., Ruslim, Lany, Artis, Dean R., Yednock, Ted A.
Format:	Artikel
Sprache:	eng
Schlagworte:	Alzheimer’s disease Amyloid Precursor Protein Secretases - antagonists & inhibitors Aspartic Acid Endopeptidases - antagonists & inhibitors BACE-1 Beta-secratase inhibitor Binding Sites Cat-D Cells, Cultured Chromane Chromans - chemistry Drug Design drugs Enzyme Inhibitors - chemical synthesis Ethylamines - chemical synthesis Ethylamines - chemistry Ethylamines - pharmacology Hydroxyethylamine in vitro studies Inhibitory Concentration 50 Models, Molecular Permeability Structure-Activity Relationship structure-activity relationships
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