Potent and selective isophthalamide S2 hydroxyethylamine inhibitors of BACE1.

Steven W Kortum, Timothy E Benson, Michael J Bienkowski, Thomas L Emmons, D Bryan Prince, Donna J Paddock, Alfredo G Tomasselli, Joseph B Moon, Alice LaBorde, Ruth E TenBrink

Index: Bioorg. Med. Chem. Lett. 17(12) , 3378-83, (2007)

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Abstract

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.