Design, Synthesis, and Crystal Structure of Hydroxyethyl Secondary Amine-Based Peptidomimetic Inhibitors of Human beta -Secretasep

The design and synthesis of a novel series of potent and cell permeable peptidomimetic inhibitors of the human beta -secretase (BACE) are described. These inhibitors feature a hydroxyethyl secondary amine isostere and a novel aromatic ring replacement for the C-terminus. The crystal structure of BAC...

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Bibliographic Details
Published in:Journal of medicinal chemistry 2007-02, Vol.50 (4), p.776-781
Main Authors: Maillard, M C, Hom, R K, Benson, TE, Moon, J B, Mamo, S, Bienkowski, M, Tomasselli, A G, Woods, D D, Prince, D B, Paddock, D J, Emmons, T L, Tucker, JA, Dappen, MS, Brogley, L
Format: Article
Language:English
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Summary:The design and synthesis of a novel series of potent and cell permeable peptidomimetic inhibitors of the human beta -secretase (BACE) are described. These inhibitors feature a hydroxyethyl secondary amine isostere and a novel aromatic ring replacement for the C-terminus. The crystal structure of BACE in complex with this hydroxyethyl secondary amine isostere inhibitor is also presented.
ISSN:0022-2623
DOI:10.1021/jm061242y