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- W2060227677 abstract "Fluorinated ketone thrombin inhibitors based on the peptide sequence methyl-(D)-Phe-Pro-Arg-CF2R were synthesized: MDL 73,446 (1, R = F); MDL 73,775 (2, R = CF3); and MDL 75,579 (3, R = CH2CH2CH3). These were shown to be highly effective, slow binding inhibitors of thrombin. Anticoagulant activity was dose-dependent with 3 > 2 > 1 at doubling thrombin time and APTT, respectively. Anticoagulant activity corresponded with efficacy in a platelet-dependent (FeCl3-induced) rat carotid artery thrombosis model. Arterial occlusion was dose-dependently prolonged with 3 > 2 > 1 at doubling the occlusion time." @default.
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- W2060227677 date "1995-08-01" @default.
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- W2060227677 title "Synthesis and comparison of tripeptidylfluoroalkane thrombin inhibitors" @default.
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- W2060227677 doi "https://doi.org/10.1016/0968-0896(95)00097-z" @default.
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