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Design, synthesis and testing of amino-bicycloaryl based orally bioavailable thrombin inhibitors
J B Rewinkel1, H Lucas, M J Smit
1NV Organon, Research and Development, Oss, The Netherlands.
Bioorganic & Medicinal Chemistry Letters
|October 16, 1999
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.