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Related Experiment Videos

[New antithrombotic oligosaccharides].

M Petitou1, J P Hérault, A Bernat

  • 1Sanofi Recherche, Ligne Hémobiologie, Toulouse.

Annales Pharmaceutiques Francaises
|July 31, 1999
PubMed
Summary
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Researchers synthesized novel oligosaccharides that act as potent antithrombotic drugs. These compounds mimic heparin's anticoagulant activity without adverse side effects, offering a potential "ideal" treatment.

Area of Science:

  • Synthetic chemistry
  • Carbohydrate chemistry
  • Pharmacology

Context:

  • Heparin's anticoagulant mechanism involves binding to antithrombin.
  • Early synthesis achieved pentasaccharides representing heparin's antithrombin binding site.
  • Selective inhibitors of coagulation factor Xa were developed.

Purpose:

  • To design and synthesize novel oligosaccharides with enhanced antithrombotic properties.
  • To create compounds that inhibit both factor Xa and thrombin via antithrombin.
  • To develop heparin-like antithrombotics devoid of non-specific interactions.

Summary:

  • Chemical synthesis of oligosaccharides has advanced, enabling the creation of heparin analogs.
  • Oligosaccharides were designed to include both antithrombin and thrombin binding domains.

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  • These synthetic compounds exhibit full anticoagulant activity, inhibiting factor Xa and thrombin.

    • Impact:

    • Developed selective inhibitors of coagulation factor Xa, a new class of antithrombotic drugs.
    • Synthesized "ideal heparin-like antithrombotics" with full anticoagulant activity.
    • Eliminated undesired non-specific interactions, such as those with platelet factor 4 (PF4).