Bioorganic and Medicinal Chemistry Letters p. 3183 - 3186 (2002)
Update date:2022-08-04
Topics:
Iwanowicz, Edwin J
Kimball
Lin, James
Lau, Wan F.
Han
Wang, Tammy C.
Roberts, Daniel G.M.
Schumacher
Ogletree, Martin L.
Seiler, Steven M.
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.
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