Chapter 16. A New Generation of Antithrombotics Based on Synthetic Oligosaccharides

  1. Prof. Dr. Chi-Huey Wong
  1. Maurice Petitou,
  2. Jean-Marc Herbert

Published Online: 28 JAN 2005

DOI: 10.1002/3527602437.ch16

Book Title

Carbohydrate-Based Drug Discovery

Carbohydrate-Based Drug Discovery

Additional Information

How to Cite

Petitou, M. and Herbert, J.-M. (2005) A New Generation of Antithrombotics Based on Synthetic Oligosaccharides, in Carbohydrate-Based Drug Discovery (ed C.-H. Wong), Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim, FRG. doi: 10.1002/3527602437.ch16

Editor Information

  1. Ernest W. Hahn Chair in Chemistry, The Scripps Research Institute, 10550 N. Torrey Pines RoadLa Jolla, CA 92037, USA

Publication History

  1. Published Online: 28 JAN 2005
  2. Published Print: 26 AUG 2003

ISBN Information

Print ISBN: 9783527306329

Online ISBN: 9783527602438

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Keywords:

  • antithrombotics;
  • synthetic oligosaccharides;
  • heparin;
  • synthetic pentasaccharides;
  • factor Xa inhibitors;
  • mechanism of antithrombin activation

Summary

  • Introduction

  • Heparin and Its Mechanism of Action as an Antithrombotic Agent

    • Heparin, a Complex Polysaccharide with Blood Anticoagulant Properties

    • Which Coagulation Factor must be Inhibited?

    • The Structure of Heparin in Relation to Antithrombin Activation

    • The Limitations of Heparin

  • Synthetic Pentasaccharides, Selective Factor Xa Inhibitors, are Antithrombotic Agents

  • New Synthetic Oligosaccharides Required in Order to Validate A Pharmacological Hypothesis

  • A Strategy for the Synthesis of an Active Pentasaccharide

  • A Strategy for the Synthesis of the First Pentasaccharide

  • Activation of Antithrombin: Structure/Activity Relationship

  • Clinical Trials Results

  • The Second Generation of Antithrombotic Pentasaccharides

  • Synthetic Thrombin-Inhibiting Oligosaccharides: The Next Generation?

    • First Approach: Oligomerization of a Disaccharide

    • Second Approach: Molecules Containing Two Identified Domains

    • Introduction of a Neutral Domain

  • The Mechanism of Antithrombin Activation by Synthetic Oligosaccharides

  • Conclusion and Perspectives

  • References

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