Bioorganic and Medicinal Chemistry
Bioorganic and Medicinal Chemistry
5 years ago

Design and synthesis of bicyclic acetals as Beta Secretase (BACE1) inhibitors

Design and synthesis of bicyclic acetals as Beta Secretase (BACE1) inhibitors
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.

Publisher URL: www.sciencedirect.com/science

DOI: S096808961730528X

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