244606-15-3Relevant articles and documents
Design and synthesis of a novel synthetic NAPAP-pentasaccharide conjugate displaying a dual antithrombotic action
Buijsman, Rogier C.,Basten, Jan E. M.,Van Dinther, Theo G.,Van der Marel, Gijsbert A.,Van Boeckel, Constant A. A.,Van Boom, Jacques H.
, p. 2013 - 2018 (1999)
The synthesis of a novel antithrombotic consisting of a heparin pentasaccharide conjugated to the active site inhibitor N-(2- naphtalenesulfonyl)-glycyl-(D)-4-aminophenyl-alanyl-piperidine (NAPAP) (i.e. compound I) is reported. This conjugate shows a unique pharmacological profile both in vitro and in vivo having direct anti-thrombin and ATIII- mediated anti-Xa activity. Furthermore, conjugate I has a prolonged in vivo half-life compared to NAPAP (1.5 h vs 9 min.).