Parameters of thrombin inhibition and acute toxicity for the best new thrombin inhibitors and argatroban1).

1)The common formula for all inhibitors is depicted in Fig. 3A.2)Synthesis details are in the Supporting Information.3)Measured by chromogenic substrate Tosyl-Gly-Pro-Arg-p-nitroanilide.4)The KI values were calculated with the assumption of a competitive type of inhibition. The KM value of the substrate for thrombin is 9.44 µM.5)Substance is nontoxic in thousand-fold ETP reduction IC50 dose (per whole mouse).6)IT contains methyl group as a substituent in one of the amino groups.7)All constants for argatroban (except for the LD50) were measured and were in good agreement with data in the literature [35]–[38].