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  • Title: Design and synthesis of bicyclic acetals as Beta Secretase (BACE1) inhibitors.
    Author: Innocenti R, Lenci E, Menchi G, Pupi A, Trabocchi A.
    Journal: Bioorg Med Chem; 2017 Oct 01; 25(19):5077-5083. PubMed ID: 28359674.
    Abstract:
    Taking advantage of the structural similarity between aspartic proteases, small-molecule peptidomimetic inhibitors that already showed activity towards Secreted Aspartic Protease 2 as anti-Candida agents and HIV protease inhibitors were exploited as potential BACE1 inhibitors. A focused library of 6,8-dioxa-3-azabicyclo[3.2.1]-octane peptidomimetic scaffolds was synthesized and assayed towards BACE1 enzyme, resulting in the identification of a thiolactam-containing hit compound possessing IC50 in the low micromolar range, and confirming the bicyclic acetal portion as a potential transition state analogue in the interaction with catalytic aspartic acid residues.
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