Chapter 1. Analogues as a Means of Discovering New Drugs

  1. Dr. János Fischer2,
  2. Prof. Dr. C. Robin Ganellin3
  1. Camille G. Wermuth

Published Online: 22 MAY 2006

DOI: 10.1002/3527608001.ch1

Book Title

Analogue-based Drug Discovery

Analogue-based Drug Discovery

Additional Information

How to Cite

Wermuth, C. G. (2006) Analogues as a Means of Discovering New Drugs, in Analogue-based Drug Discovery (eds J. Fischer and C. R. Ganellin), Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim, FRG. doi: 10.1002/3527608001.ch1

Editor Information

  1. 2

    Gedeon Richter Ltd., P.O. Box 27, H-1475 Budapest 10, Hungary

  2. 3

    University College London, Department of Chemistry, 20 Gordon Street, London WC1H OAJ, UK

Author Information

  1. Prestwick Chemical Inc., Boulevard Gonthier d'Andernach, Strasbourg Innovation Park, 67400 Illkirch Cedex, France

Publication History

  1. Published Online: 22 MAY 2006
  2. Published Print: 20 JAN 2006

ISBN Information

Print ISBN: 9783527312573

Online ISBN: 9783527608003

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CHAPTER TOOLS

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Keywords:

  • analogue-based drug discovery;
  • designing of analogues;
  • vinylogy;
  • isosteric variations;
  • positional isomers;
  • optical isomers;
  • ring transformations;
  • twin drugs;
  • pros and cons of analogue design

Summary

This chapter contains sections titled:

  • Designing of Analogues

    • Analogues Produced by Homologous Variations

      • Homology Through Monoalkylation

      • Polymethylenic Bis-Ammonium Compounds: Hexa- and Decamethonium

      • Homology in Cyclic Compounds

    • Analogues Produced by Vinylogy

      • Zaprinast Benzologues

    • Analogues Produced by Isosteric Variations

      • The Dominant Parameter is Structural

      • The Dominant Parameter is Electronic

      • The Dominant Parameter is Lipophilicity

    • Positional Isomers Produced as Analogues

    • Optical Isomers Produced as Analogues

      • Racemic Switches

      • Specific Profile for Each Enantiomer

    • Analogues Produced by Ring Transformations

    • Twin Drugs

  • The Pros and Cons of Analogue Design

    • The Success is Almost Warranted

    • The Information is Available

    • Financial Considerations

    • Emergence of New Properties

  • Analogue Design as a Means of Discovering New Drugs

    • New Uses for Old Drugs

    • The PASS Program

    • New Leads from Old Drugs: The SOSA Approach

      • Definition

      • Rationale

      • Availability

      • Examples

      • Discussion

  • Conclusion

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