1-Aminoisoquinoline as benzamidine isoster in the design and synthesis of orally active thrombin inhibitors.

1-Aminoisoquinoline as benzamidine isoster in the design and synthesis of orally active thrombin inhibitors.

Bioorganic & medicinal chemistry letters (1999-04-14)

J B Rewinkel, H Lucas, P J van Galen, A B Noach, T G van Dinther, A M Rood, A J Jenneboer, C A van Boeckel

PMID10201829

RÉSUMÉ

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.