Description

Progress in Medicinal Chemistry provides a review of eclectic developments in medicinal chemistry. This volume continues in the serial's tradition of providing an insight into the skills required of the modern medicinal chemist; in particular, the use of an appropriate selection of the wide range of tools now available to solve key scientific problems.

Key Features

  • Progress in Medicinal Chemistry provides a review of eclectic developments in medicinal chemistry
  • This volume continues in the serial's tradition of providing an insight into the skills required of the modern medicinal chemist; in particular, the use of an appropriate selection of the wide range of tools now available to solve key scientific problems

Readership

Chemists, biologists, doctors, pharmacists and anyone interested in the contemporary controversy about drugs, drug firms, and the community

Table of Contents

  • Preface
  • Contributors
  • Chapter One. Property-Based Design in the Optimisation of Benzamide Glucokinase Activators
    • 1. Introduction
    • 2. Hit-to-Lead SAR—Improving Chemical and Metabolic Stability
    • 3. Balancing Potency, Lipophilicity and Free Drug to Deliver an In Vivo Tool Compound
    • 4. Structural Basis for Small-Molecule Activation
    • 5. Optimising Pharmacokinetics by Focussing on Unbound Clearance
    • 6. Defining a Pharmacokinetic–Pharmacodynamic Relationship
    • 7. Testicular Toxicology and the Role of RAR-α Antagonism
    • 8. Defining Molecular Descriptor Criteria to Improve Success Rates Against Key Optimisation Parameters
    • 9. Overcoming Challenges Associated with Crystallinity and Physical Form
    • 10. Profile of Clinical Candidate AZD1092
    • 11. Risk Mitigation—Remit and Strategy for Backup Campaign
    • 12. Mitigating Fragment Mutagenicity Concerns and Developing a Predictive Model for Ames Activity
    • 13. Moderating H-Bond Donor Count to Improve Absorption
    • 14. Re-balancing Lipophilicity by Incorporation of Polar Heterocycles
    • 15. Identification and Profile of Clinical Candidate AZD1656
    • 16. Synthesis of Benzamide GKAs
    • 17. Summary and Future Perspectives
    • References
  • Chapter Two. Medicinal Chemistry of Glucagon-Like Peptide Receptor Agonists
    • 1. Introduction
    • 2. The Incretin Concept and Diabetes
    • 3. Structure–Activity Relationships of the GLP-1 Peptide
    • 4. Exendin-4 and Exenatide
    • 5. Exenatide ER
    • 6. Liraglutide
    • 7. Non-Lipophilic Acid Conjugates
    • 8. Alternative Routes of Administration
    • 9. Inhaled GLP-1 Agonists
    • 10. Alternative Indications
    • 11. Conclusions
    • References
    • Further Reading
  • Chapter Three. Antimalarial Drug Discovery

Details

No. of pages:
264
Language:
English
Copyright:
© 2013
Published:
Imprint:
Elsevier
eBook ISBN:
9780444626714
Print ISBN:
9780444626523