Document Report Card

Basic Information

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

DOI: 10.1016/s0960-894x(02)00651-0