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United States Patent 6,326,492
<<Thrombin: Thrombin activity was assessed as the ability to hydrolyze the substrate N-succinyl-Ala-Ala-Pro-Arg-p-nitroanilide. Substrate solutions were prepared at a concentration of 32 mM (32 mM<<Km=180 mM) in assay buffer. Final DMSO concentration was 4.3%. Purified human a-thrombin was diluted into assay buffer to a concentration of 15 nM. Final reagent concentrations were: [thrombin]=0.5 nM, [substrate N-succinyl-Ala-Ala-Pro-Arg-p-nitroanilide]=32 mM.
The compound of Example 1 had a thrombin inhibitory activity of 26 nM. The compound of Example 2 had a thrombin inhibitory activity of 0.38 nM. The results indicate that the compounds of the present invention are potent and highly selective inhibitors of thrombin.>>