Imants Kreituss

Discovery of aziridine-triazole conjugates as selective MMP-2 inhibitors

A series of (aryltriazolyl)methylaziridines was synthesized and evaluated as selective inhibitors of matrix metalloproteinase-2. They constitute a novel class of hydroxamic acid-free matrix metalloproteinase inhibitors. The triazole fragment serves as a linker between the hydrophilic aziridine and the lipophilic part of the molecule. The best inhibition was observed with 1-(aziridin-2-ylmethyl)-4-(4-butylphenyl)-1H-1,2,3-triazole and 1-(aziridin-2-ylmethyl)-4-phenyl-1H-1,2,3-triazole that selecti-vely inhibited metalloproteinase-2 at 73% in 20 μM concentration and at 75% in 10 μM concentration, respectively.