3,1-Benzothiazines, 1,4-benzodioxines, 1,4-benzoxazines as inhibitors of matriptase-2Roydeva, Polya G. (Avtor) Beckmann, Anna-Madeleine (Avtor) Stirnberg, Marit (Avtor) Cesar, Jožko (Avtor) Kikelj, Danijel (Avtor) Ilaš, Janez (Avtor) Gütschow, Michael (Avtor) marine alkaloidAgelasclathrodinoroidinpyrrole-2-aminoimidazoleantibacterialbenzamidines4H-31-benzothiazin-4-ones23-dihydro-14-benzodioxines34-dihydro-2H-14-benzoxazinesmatriptase-2protease inhibitionThe 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.20162021-09-14 10:35:11Članek v reviji130387sl