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  • Title: Design, synthesis and testing of amino-bicycloaryl based orally bioavailable thrombin inhibitors.
    Author: Rewinkel JB, Lucas H, Smit MJ, Noach AB, van Dinther TG, Rood AM, Jenneboer AJ, van Boeckel CA.
    Journal: Bioorg Med Chem Lett; 1999 Oct 04; 9(19):2837-42. PubMed ID: 10522702.
    Abstract:
    Replacement of the highly basic benzamidine moiety with moderate basic amino-bicycloaryl moieties in a series of thrombin inhibitors related to NAPAMP provided potent enzyme inhibition and significant improvements in membrane transport and oral bioavailability.
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