Author/Authors :
Edwin J. Iwanowicz، نويسنده , , S. David Kimball، نويسنده , , Ming-Ji James Lin، نويسنده , , Wan F. Lau، نويسنده , , W. -S. Han، نويسنده , , Tammy C. Wang، نويسنده , , Daniel G. M. Roberts، نويسنده , , W. A. Schumacher، نويسنده , , Martin L. Ogletree، نويسنده , , Steven M. Seiler، نويسنده ,
Abstract :
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.