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  • Title: Fluoro-olefins as peptidomimetic inhibitors of dipeptidyl peptidases.
    Author: Van der Veken P, Senten K, Kertèsz I, De Meester I, Lambeir AM, Maes MB, Scharpé S, Haemers A, Augustyns K.
    Journal: J Med Chem; 2005 Mar 24; 48(6):1768-80. PubMed ID: 15771423.
    Abstract:
    The feasibility of the fluoro-olefin function as a peptidomimetic group in inhibitors for dipeptidyl peptidase IV and II (DPP IV and DPP II) is investigated by evaluation of N-substituted Gly-Psi[CF=C]pyrrolidines, Gly-Psi[CF=C]piperidines, and Gly-Psi[CF=C](2-cyano)pyrrolidines. Of this later class, the (Z)- and (E)-fluoro-olefin analogues were prepared and chemical stability in comparison with the parent amide was checked. Most of these compounds exhibited a strong binding preference toward DPP II with IC(50) values in the low micromolar range, while only low DPP IV inhibitory potential is seen.
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