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  • Title: Identification of constrained peptidomimetic chemotypes as HIV protease inhibitors.
    Author: Calugi C, Guarna A, Trabocchi A.
    Journal: Eur J Med Chem; 2014 Sep 12; 84():444-53. PubMed ID: 25042102.
    Abstract:
    Small-molecule peptidomimetic inhibitors that already showed activity towards Secreted aspartic protease 2 as anti-Candida agents are herein presented as candidate HIV protease inhibitors. A library of 6,8-dioxa-3-azabicyclo[3.2.1]-octane peptidomimetic scaffolds was screened towards HIV protease, resulting in the identification of hit compounds possessing IC50 in the sub-micromolar range, and showing the bicyclic acetal portion as a potential transition state analogue in the interaction with catalytic aspartic acid residues.
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