Author/Authors :
M. L. Quan، نويسنده , , J. R. Pruitt، نويسنده , , C. D. Ellis، نويسنده , , A. Y. Liauw، نويسنده , , R. A. Galemmo Jr.، نويسنده , , P. F. W. Stouten، نويسنده , , J. Wityak، نويسنده , , R. M. Knabb، نويسنده , , M. J. Thoolen، نويسنده , , P. C. Wong، نويسنده , , R. R. Wexler، نويسنده ,
Abstract :
Factor Xa is an important serine protease in the blood coagulation cascade. It generates thrombin and holds the central position that links the intrinsic and extrinsic activation mechanism in the final common pathway of coagulation. Therefore, inhibition of factor Xa has potential therapeutic applications in the treatment of both arterial and venous thrombosis. We have designed and synthesized a series of bisbenzamidine isoxazoline derivatives as factor Xa inhibitors. The most potent compound in this series has a Ki of 18 nM against factor Xa.
