Design, synthesis, and in vitro biological activity of indole-based factor Xa inhibitors

…, A Liang, L Trinh, M Whitlow, SK Koovakkat…

Index: Arnaiz, Damian O.; Zhao, Zuchun; Liang, Amy; Trinh, Lan; Whitlow, Marc; Koovakkat, Sunil K.; Shaw, Kenneth J. Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 9 p. 957 - 961

Full Text: HTML

Citation Number: 13

Abstract

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 ...