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  • Title: 1-Aminoisoquinoline as benzamidine isoster in the design and synthesis of orally active thrombin inhibitors.
    Author: Rewinkel JB, Lucas H, van Galen PJ, Noach AB, van Dinther TG, Rood AM, Jenneboer AJ, van Boeckel CA.
    Journal: Bioorg Med Chem Lett; 1999 Mar 08; 9(5):685-90. PubMed ID: 10201829.
    Abstract:
    Replacement of the highly basic benzamidine moiety of NAPAP by the moderately basic 1-aminoisoquinoline moiety resulted in thrombin inhibitors with improved selectivity towards trypsin and enhanced Caco-2 cell permeability.
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