Design, synthesis and testing of amino-bicycloaryl based orally bioavailable thrombin inhibitors

Article abstract of DOI:10.1016/S0960-894X(99)00483-7

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.