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J Med Chem. 2005 Apr 7;48(7):2266-9.

3-Substituted imidazo[1,2-d][1,2,4]-thiadiazoles: a novel class of factor XIIIa inhibitors.

Author information

1
Department of Medicinal Chemistry, Apotex Research Inc., 400 Ormont Drive, Toronto, ON M9L 1N9, Canada.

Abstract

A new class of selective FXIIIa inhibitors with a bicyclic [1,2,4]-thiadiazole pharmacophore is described. At 160 muM, compound 8 caused 50% reduction in fibrin gamma-chain cross-linking and suppressed the polymerization of alpha 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.

PMID:
15801818
DOI:
10.1021/jm049221w
[Indexed for MEDLINE]

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