Retro-binding thrombin active site inhibitors: Identification of an orally active inhibitor of thrombin catalytic activity

Article abstract of DOI:10.1016/S0960-894X(02)00651-0

A series of retro-binding inhibitors of human α-thrombin was prepared to elucidate structure-activity relationships (SAR) and optimize in vivo performance. Compounds 9 and 11, orally active inhibitors of thrombin catalytic activity, were identified to be efficacious in a thrombin-induced lethality model in mice.