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  • Title: Inhibitors of dipeptidyl peptidase 8 and dipeptidyl peptidase 9. Part 1: identification of dipeptide derived leads.
    Author: Van der Veken P, De Meester I, Dubois V, Soroka A, Van Goethem S, Maes MB, Brandt I, Lambeir AM, Chen X, Haemers A, Scharpé S, Augustyns K.
    Journal: Bioorg Med Chem Lett; 2008 Jul 15; 18(14):4154-8. PubMed ID: 18556199.
    Abstract:
    Dipeptide derivatives bearing various P2 residues and pyrrolidine derivatives as P1 mimics were evaluated in order to identify lead structures for the development of DPP8 and DPP9 inhibitors. Structure-activity-relationship data obtained in this way led to the preparation of a series of alpha-aminoacyl ((2S, 4S)-4-azido-2-cyanopyrrolidines). These compounds were shown to be nanomolar DPP8/9 inhibitors with modest overall selectivity toward DPP IV and DPP II.
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