3-Substituted Imidazo[1,2-d][1,2,4]-thiadiazoles: A Novel Class of Factor XIIIa Inhibitors
journal contributionposted on 07.04.2005, 00:00 by Regis Leung-Toung, Tim F. Tam, Jolanta M. Wodzinska, Yanqing Zhao, Jayme Lowrie, Craig D. Simpson, Khashayar Karimian, Michael Spino
A 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.