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  • Synthesis and evaluation of spumigin analogues library with thrombin inhibitory activity [Elektronski vir]
    Žula, Aleš ...
    Spumigins are marine natural products derived from cyanobacteria Nodularia spumigena, which mimics the structure of the D-Phe-Pro-Arg sequence and is crucial for binding to the active site of serine ... proteases thrombin and factor Xa. Biological evaluation of spumigins showed that spumigins with a (2S,4S)-4-methylproline central core represent potential lead compounds for the development of a new structural type of direct thrombin inhibitors. Herein, we represent synthesis and thrombin inhibitory activity of a focused library of spumigins analogues with indoline ring or L-proline as a central core. Novel compounds show additional insight into the structure and biological effects of spumigins. The most active analogue was found to be a derivative containing L-proline central core with low micromolar thrombin inhibitory activity.
    Vir: Marine drugs [Elektronski vir]. - ISSN 1660-3397 (Vol. 16, iss. 11, Nov. 2018, str. 1-19)
    Vrsta gradiva - e-članek
    Leto - 2018
    Jezik - angleški
    COBISS.SI-ID - 39787781

    Povezava(-e):

    https://www.mdpi.com/1660-3397/16/11/413
    Repozitorij Univerze v Ljubljani – RUL
    DOI

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