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Progress in Medicinal Chemistry - 1st Edition - ISBN: 9780444626523, 9780444626714

Progress in Medicinal Chemistry, Volume 52

1st Edition

Serial Editors: G. Lawton David Witty
Hardcover ISBN: 9780444626523
eBook ISBN: 9780444626714
Imprint: Elsevier
Published Date: 1st March 2013
Page Count: 264
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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
    • 1. Introduction
    • 2. Antimalarial Drugs Inhibiting Defined Molecular Targets
    • 3. Antimalarial Drugs with a Complex Mode of Action
    • 4. Current Approaches for Antimalarial Lead Discovery
    • 5. New Areas of Investigation for Antimalarial Therapies: Exoerythrocytic Stages
    • 6. Conclusion
    • References
  • Chapter Four. Advances in the Discovery of Selective JAK Inhibitors
    • 1. Introduction
    • 2. Biology Background
    • 3. JAK Inhibitors and Progress Towards Subtype Selectivity
    • 4. Structural Biology of the JAK Kinase Family
    • 5. Approved Drugs and Those in Clinical Trial
    • 6. Conclusion
    • References
  • Subject Index
  • Cumulative Index of Authors for Volumes 1–52
  • Cumulative Index of Subjects for Volumes 1–52


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


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


No. of pages:
© Elsevier 2013
1st March 2013
Hardcover ISBN:
eBook ISBN:

Ratings and Reviews

About the Serial Editors

G. Lawton

G. Lawton

Dr Geoff Lawton has extensive experience in new medicine discovery across many therapeutic areas in both large and small companies and is a co-inventor of a marketed drug (Cilazapril). He is a former Director of Chemistry at Roche UK, and Vice-president Chemistry and Preclinical Sciences within Roche Bioscience, Palo Alto, USA. He was for five years the research member of a global therapy area strategy planning team for inflammatory diseases, aligning research with the clinical development and marketing parts of the business.

From 2003 to 2007 he was founding Research Director with Lectus Therapeutics building from start-up a drug discovery organisation; generating the team, facilities and project portfolio targeting the next generation of ion channel modulating medicines.

Since 2001 Geoff has provided scientific and strategic evaluation and advice on drug discovery as an independent consultant for a number small and medium sized biotech companies, CROs, VCs, academic groups and medical research charities.

Geoff serves on the Board of Antabio, a French biotech company developing tomorrow’s antibacterial drugs.

He is a founder of INMedD, a new medicines discovery social enterprise.

Affiliations and Expertise

St. Ippolyts, Herts, UK

David Witty

David Witty

Dr David Witty has more than 20 years experience in the pharmaceutical industry as a medicinal chemist and project leader working principally in areas of anti-infectives, metabolic diseases, cognition and pain, delivering clinical candidates for several conditions. He led IT Strategy within the Neurology division of GSK, developing and deploying the first Electronic Notebooks for drug discovery to sites in the UK and Singapore. He has contributed more than 90 scientific papers, reviews, patents and books on medicinal and synthetic chemistry.

In 2010 David and several colleagues successfully raised $35M in venture funding to found Convergence Pharmaceuticals, a specialist ion channel company focused on the development of novel treatments for pain, based in Cambridge UK. David presently leads their discovery programme and manages scientific operations within the business.

David is chairman of the Fine Chemicals Group of the Society of Chemical Industry, with responsibility for the delivery of conferences, seminars and training courses for chemists throughout the UK and Europe, and advising parliamentary bodies on matters of relevance to the UK chemical industry.

Since 2008 David has been a STEM ambassador for SETPOINT, introducing school students at both primary and secondary level to the excitement and possibilities of pursuing scientific careers, through workshops, lectures and competitions.

Affiliations and Expertise

WITNET LTD, Cambridge, UK