Early studies in our laboratory led to the identification of Z,Z-2,7-bis-(4-amidinobenzylidene) cycloheptanone (Z,Z-BABCH, 1) as the active isomer in a series of conformationally rigid bis-benzamidine inhibitors (Fig. 1). 3 Z,Z-BABCH inhibits human FXa with a K i of 0.66 nM, but has limited potential for development due to its photochemical instability. We sought to replace the cycloheptanone core of 1 with stable scaffolds that could maintain the U-shaped ...
