Chapter 18. The Development of Bisphosphonates as Drugs

  1. Dr. János Fischer2,
  2. Prof. Dr. C. Robin Ganellin3
  1. Eli Breuer

Published Online: 22 MAY 2006

DOI: 10.1002/3527608001.ch18

Book Title

Analogue-based Drug Discovery

Analogue-based Drug Discovery

Additional Information

How to Cite

Breuer, E. (2006) The Development of Bisphosphonates as 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.ch18

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. The Hebrew University of Jerusalem, School of Pharmacy, Department of Medicinal Chemistry, P.O. Box 12065, 91120 Jerusalem, Israel

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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Keywords:

  • analogue-based drug discovery;
  • development of bisphosphonates as drugs;
  • biological activity of pyrophosphate;
  • biological activity of bisphosphonates;
  • bone-related activity;
  • miscellaneous biological aspects of bisphosphonates

Summary

This chapter contains sections titled:

  • Historical Background

  • Discovery of the Biological Activity of Pyrophosphate and of Bisphosphonates

  • Bone-Related Activity of Bisphosphonates

    • Overview

    • Osteolytic Bone Diseases

      • Osteoporosis

      • Osteolytic Tumors

      • Paget's Disease

    • Structure-Activity Relationships

      • The Molecular Skeletons of Bisphosphonates

      • Phosphonic Acid Groups

      • The Geminal Hydroxy Group

      • Nitrogen-Containing Side Chain

      • Structure-Activity Relationships of BPs: A Summary

    • Inhibition of Bone Resorption: The Mechanisms of Action

    • Clinical Pharmacology of Bisphosphonates

    • Bisphosphonates in Clinical Use

  • Miscellaneous Biological Aspects of Bisphosphonates

    • Bisphosphonates as Vehicles for Delivering Drugs to Bone

    • Bisphosphonates as Potential Drugs for other Indications

      • Antiviral Drugs

      • Bisphosphonate Inositol-Monophosphatase Inhibitor: A Potential Drug for Bipolar Disorders

      • Hypocholesterolemic Bisphosphonates (Squalene Synthase Inhibitors)

      • Antiparasitic Drugs

      • Anti-Inflammatory and Anti-Arthritic Bisphosphonates

      • Cardiovascular Applications of Bisphosphonates

  • Conclusions

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