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ID: ALA1134950
Journal: Bioorg Med Chem Lett
Title: Retro-binding thrombin active site inhibitors: identification of an orally active inhibitor of thrombin catalytic activity.
Authors: Iwanowicz EJ, Kimball SD, Lin J, Lau W, Han WC, Wang TC, Roberts DG, Schumacher WA, Ogletree ML, Seiler SM.
Abstract: A series of retro-binding inhibitors of human alpha-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.
CiteXplore: 12372529