Author/Authors :
Yong Gong، نويسنده , , Henry W. Pauls، نويسنده , , Alfred P. Spada، نويسنده , , Mark Czekaj، نويسنده , , Guyan Liang، نويسنده , , Valeria Chu، نويسنده , , Dennis J. Colussi، نويسنده , , Karen D. Brown، نويسنده , , Jingbo Gao، نويسنده ,
Abstract :
The design, synthesis and SAR of amido-(propyl and allyl)-hydroxybenzamidine coagulation factor Xa inhibitors is described. These achiral inhibitors are selective for fXa vis a vis structurally related serine proteases and are readily prepared in 6–7 linear steps. The most potent member 9j (fXa Ki=0.75 nM) is selective (>1000-fold) and an effective anticoagulant in mammalian plasma.
