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Design of potent inhibitors of human beta-secretase. Part 1
Authors:Freskos John N  Fobian Yvette M  Benson Timothy E  Bienkowski Michael J  Brown David L  Emmons Thomas L  Heintz Robert  Laborde Alice  McDonald Joseph J  Mischke Brent V  Molyneaux John M  Moon Joseph B  Mullins Patrick B  Bryan Prince D  Paddock Donna J  Tomasselli Alfredo G  Winterrowd Gregory
Affiliation:Pfizer Inc., 700N. Chesterfield Pkwy., St. Louis, MO 63198, USA. john.n.freskos@pfizer.com
Abstract:We describe a novel series of potent inhibitors of human beta-secretase. These compounds possess the hydroxyethyl amine transition state isostere. A 2.5A crystal structure of inhibitor 32 bound to BACE is provided.
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