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2007•Journal of Medicinal ChemistryOpen access

Design, Synthesis, and Crystal Structure of Hydroxyethyl Secondary Amine-Based Peptidomimetic Inhibitors of Human β-Secretase

Michel Maillard, Roy K. Hom, Timothy E. Benson, Joseph B. Moon, Shumeye Mamo, Michael J. Bienkowski, Alfredo G. Tomasselli, Danielle D. Woods, D. Bryan Prince, Donna J. Paddock, Thomas L. Emmons, John A. Tucker, Michael S. Dappen, Louis Brogley, Eugene D. Thorsett, Nancy Jewett, Sukanto Sinha, Varghese John

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Abstract

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.

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What this paper is about

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.

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Available abstract

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.

Key concepts: Peptidomimetic, Isostere, Chemistry, Amine gas treating, Stereochemistry, Tertiary amine, Combinatorial chemistry, Biochemistry

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Design, Synthesis, and Crystal Structure of Hydroxyethyl Secondary Amine-Based Peptidomimetic Inhibitors of Human β-Secretase — Research Paper | ScholarLens