Annual Reports in Medicinal Chemistry, Volume 47

1st Edition

Series Editors: John Macor
Paperback ISBN: 9780123964922
eBook ISBN: 9780123972149
Imprint: Academic Press
Published Date: 8th October 2012
Page Count: 472
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Table of Contents



Chapter One Reflections on Medicinal Chemistry at Merck, West Point

Chapter Two My Path in Seeking New Medicines


Chapter Three Tales of Drug Discovery

1 Prostaglandins

2 Cannabinoid Analgesics

3 Hypoglycemic Agents

4 Opioid Analgesics

5 HIV Fusion Inhibitors

6 Epithelial Sodium Channel Blockers

7 Conclusions and Ramblings

Chapter Four Recent Developments in Targeting Neuroinflammation in Disease

1 Introduction

2 Ion Channels

3 Enzymes

4 Receptors

5 Concluding Remarks

Chapter Five Secretase Inhibitors and Modulators as a Disease-Modifying Approach Against Alzheimer’s Disease

1 Introduction

2 Inhibitors of GS

3 Modulators of GS

4 Inhibitors of β-Secretase

5 Concluding Remarks

Chapter Six mGluR2 Activators and mGluR5 Blockers Advancing in the Clinic for Major CNS Disorders

1 Introduction

2 Discovery and Development of mGluR2 Activators

3 Drug Discovery and Development of mGluR5 NAMs

4 Conclusion

Chapter Seven NMDA Antagonists of GluN2B Subtype and Modulators of GluN2A, GluN2C, and GluN2D Subtypes—Recent Results and Developments

1 Introduction

2 X-ray Structural Studies and Homology Modeling of NMDA Receptors

3 Channel Blockers

4 Inhibitors of GluN2B Subtype Receptor

5 Inhibitors and Modulators of GluN2A, GluN2C, and GluN2D Subtype Receptors

6 Clinical Trials

7 Conclusions

Chapter Eight Recent Advances in the Development of PET and SPECT Tracers for Brain Imaging

1 Introduction


3 CNS PET Tracers: General Requirements and Key Hurdles

4 Recent Advances in CNS PET Tracer Development

5 New CNS PET Tracers

6 SPECT in Brain Imaging

7 Conclusions

Chapter Nine Case


Annual Reports in Medicinal Chemistry provides timely and critical reviews of important topics in medicinal chemistry together with an emphasis on emerging topics in the biological sciences, which are expected to provide the basis for entirely new future therapies.

Key Features

  • Timely and critical reviews of important topics in medicinal chemistry


Medicinal, pharmaceutical, and organic chemists


No. of pages:
© Academic Press 2012
Academic Press
eBook ISBN:
Paperback ISBN:


This series is one of the very few annual publications which justify the title of an absolute must for the pharmacologist, chemist, or physician who is interested in the chemistry of drug development." --Enzymologia

About the Series Editors

John Macor Series Editor

Affiliations and Expertise

Neuroscience Discovery Chemistry, Bristol-Myers Squibb, USA