Literature DB >> 10450972

Design and synthesis of a novel synthetic NAPAP-penta-saccharide conjugate displaying a dual antithrombotic action.

R C Buijsman1, J E Basten, T G van Dinther, G A van der Marel, C A van Boeckel, J H van Boom.   

Abstract

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-piperidin e (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.).

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Year:  1999        PMID: 10450972     DOI: 10.1016/s0960-894x(99)00320-0

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  Specificity and selectivity profile of EP217609: a new neutralizable dual-action anticoagulant that targets thrombin and factor Xa.

Authors:  Steven T Olson; Richard Swanson; Maurice Petitou
Journal:  Blood       Date:  2011-12-05       Impact factor: 22.113

2.  First in man study of EP217609, a new long-acting, neutralisable parenteral antithrombotic with a dual mechanism of action.

Authors:  Pierre Gueret; S Combe; C Krezel; E Fuseau; P L M van Giersbergen; M Petitou; E Neuhart
Journal:  Eur J Clin Pharmacol       Date:  2016-06-03       Impact factor: 2.953

3.  Long-lasting enfuvirtide carrier pentasaccharide conjugates with potent anti-human immunodeficiency virus type 1 activity.

Authors:  Thierry Huet; Olivier Kerbarh; Dominique Schols; Pascal Clayette; Cécile Gauchet; Guy Dubreucq; Loïc Vincent; Heidi Bompais; Romain Mazinghien; Olivier Querolle; Arnaud Salvador; Jérôme Lemoine; Bruno Lucidi; Jan Balzarini; Maurice Petitou
Journal:  Antimicrob Agents Chemother       Date:  2009-10-05       Impact factor: 5.191

  3 in total

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