Author/Authors :
Stephen P. O’Connor، نويسنده , , Karnail Atwal، نويسنده , , Chi Li، نويسنده , , Eddie C. -K. Liu، نويسنده , , Steven M. Seiler، نويسنده , , Mengxiao Shi، نويسنده , , Yan Shi، نويسنده , , Philip D. Stein، نويسنده , , Ying Wang، نويسنده ,
Abstract :
A series of acylguanidine derivatives were prepared and investigated as inhibitors of Factor Xa (FXa). These compounds were made by guanidine acylation with carboxylic acids using carbonyl diimidazole (CDI) as the coupling reagent. Conditions for the rapid synthesis and purification of these compounds are described along with their ability to inhibit FXa. The best FXa inhibitor is 1 with a FXa IC50 of 6 nM.
