jm049221w_si_001.pdf (551.6 kB)
3-Substituted Imidazo[1,2-d][1,2,4]-thiadiazoles: A Novel Class of Factor XIIIa Inhibitors
journal contribution
posted on 2005-04-07, 00:00 authored by Regis Leung-Toung, Tim F. Tam, Jolanta M. Wodzinska, Yanqing Zhao, Jayme Lowrie, Craig D. Simpson, Khashayar Karimian, Michael SpinoA new class of selective FXIIIa inhibitors with a
bicyclic [1,2,4]-thiadiazole pharmacophore is described. At 160
μM, compound 8 caused 50% reduction in fibrin γ-chain cross-linking and suppressed the polymerization of α chains in
platelet-depleted human plasma clots. Fibrinolysis rates in
response to tissue plasminogen activator were directly proportional to the concentration of 8 in plasma at the time of
clotting.
