Synthesis of heparin-like antithrombotics having perphosphorylated thrombin binding domains

RC Buijsman, JEM Basten, CM Dreef-Tromp…

Index: Buijsman, Rogier C.; Basten, Jan E. M.; Dreef-Tromp, Cornelia M.; Van Der Marel, Gijsbert A.; Van Boeckel, Constant A. A.; Van Boom, Jacques H. Bioorganic and Medicinal Chemistry, 1999 , vol. 7, # 9 p. 1881 - 1890

Full Text: HTML

Citation Number: 18

Abstract

The synthesis of three heparin analogues (ie compounds VI–VIII) having perphosphorylated thrombin binding domains (TBDs) is reported. These compounds were tested in vitro for their antithrombin III (ATIII)-mediated anti-Xa and antithrombin activities. Conjugates VI and VIII show a remarkable increase in antithrombin activity compared to the structurally related conjugates with persulfated TBDs (ie compounds IV and V), whereas compound VII ...