20.500.12556/RUL-125357 Synthesis and evaluation of spumigin analogues library with thrombin inhibitory activity 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. marine products natural peptides peptidomimetics thrombin inhibition biokemija morski proizvodi naravni peptidi inhibicija trombina true false true Angleški jezik Slovenski jezik Članek v reviji 2021-03-12 10:22:41 2021-03-12 10:22:43 2022-10-12 13:34:19 0000-00-00 00:00:00 2018 0 0 20 str. iss. 11, art. 413 Vol. 16 2018 0000-00-00 Zaloznikova Objavljeno NiDoloceno 0000-00-00 0000-00-00 0000-00-00 577 1660-3397 10.3390/md16110413 39787781 23578841 RAZ_Zula_Ales_2018.pdf RAZ_Zula_Ales_2018.pdf 1 28C57CB17CE81DBDBBE2E845F3FB12EE 8ed8fbbf8cab250113170c532d843c6ddfebf78ffcce15e43bd919d8d58f9aa3 b1d1ee5b-a1bb-11eb-a523-00155dcfd717 https://repozitorij.uni-lj.si/Dokument.php?lang=slv&id=141042 https://www.mdpi.com/1660-3397/16/11/413 1 https://repozitorij.uni-lj.si/Dokument.php?lang=slv&id=141044 Fakulteta za farmacijo 0 0 0