Potent and selective isophthalamide S sub(2) hydroxyethylamine inhibitors of BACE1

Potent and selective isophthalamide S sub(2) hydroxyethylamine inhibitors of BACE1

The design and synthesis of a novel series of potent BACE1 hydroxyethylamine inhibitors. These inhibitors feature hydrogen bonding substituents at the C-5 position of the isophthalamide ring with improved selectivity over cathepsin D.

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2007-06, Vol.17 (12), p.3378-3383
Hauptverfasser: Kortum, Steven W, Benson, Timothy E, Bienkowski, Michael J, Emmons, Thomas L, Prince, DBryan, Paddock, Donna J, Tomasselli, Alfredo G, Moon, Joseph B, LaBorde, Alice, TenBrink, Ruth E
Format: Artikel
Sprache:eng
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Zusammenfassung:The design and synthesis of a novel series of potent BACE1 hydroxyethylamine inhibitors. These inhibitors feature hydrogen bonding substituents at the C-5 position of the isophthalamide ring with improved selectivity over cathepsin D.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.03.096