20.500.12556/RUL-130387 3,1-Benzothiazines, 1,4-benzodioxines, 1,4-benzoxazines as inhibitors of matriptase-2 outcome of a focused screening approach The liver enzyme matriptase-2 is a multi-domain, transmembrane serine protease with an extracellular, C-terminal catalytic domain. Synthetic low-molecular weight inhibitors of matriptase-2 have potential as therapeutics to treat iron overload syndromes, in particular in patients with β-thalassemia. A sub-library of 64 compounds was screened for matriptase-2 inhibition and several active compounds were identified. (S)-Ethyl 2-(benzyl(3-((4-carbamidoylphenoxy)methyl)-2,3-dihydrobenzo[b][1,4]dioxin-6-yl)amino)-2-oxoacetate ((S)-12) showed an IC$_{50}$ value of less than 10 µM. Structure-activity relationships were discussed and proposals to design new matriptase-2 inhibitors were made. marine alkaloid Agelas clathrodin oroidin pyrrole-2-aminoimidazole antibacterial benzamidines 4H-3 1-benzothiazin-4-ones 2 3-dihydro-1 4-benzodioxines 3 4-dihydro-2H-1 4-benzoxazines matriptase-2 protease inhibition true false true Angleški jezik Ni določen Članek v reviji 2021-09-14 10:35:11 2021-09-14 10:35:12 2022-09-09 04:16:12 0000-00-00 00:00:00 2016 0 0 11 str. iss. 1, art. 2 Vol. 9 2016 0000-00-00 Zaloznikova Objavljeno NiDoloceno 0000-00-00 0000-00-00 0000-00-00 543:615.2 1424-8247 10.3390/ph9010002 4018289 RAZ_Roydeva_Polya_G._2016.pdf RAZ_Roydeva_Polya_G._2016.pdf 1 9208BD180463A4E82F3D3121DEEC33CF ee226362f85d46c794e125b6a818fdc7c2e19ee3a544c783b19d30422dd1f4a5 c03b3224-1536-11ec-a523-00155dcfd717 https://repozitorij.uni-lj.si/Dokument.php?lang=slv&id=147490 http://www.mdpi.com/1424-8247/9/1/2 0 6cf4ff5f-1536-11ec-a523-00155dcfd717 https://repozitorij.uni-lj.si/Dokument.php?lang=slv&id=147489 Fakulteta za farmacijo 0 0 0