664375-46-6Relevant academic research and scientific papers
Design and synthesis of bicyclic acetals as Beta Secretase (BACE1) inhibitors
Innocenti, Riccardo,Lenci, Elena,Menchi, Gloria,Pupi, Alberto,Trabocchi, Andrea
, p. 5077 - 5083 (2017)
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.
