Annual Reports in Medicinal Chemistry - 1st Edition - ISBN: 9780120405411, 9780080467412

Annual Reports in Medicinal Chemistry, Volume 41

1st Edition

Serial Editors: Anthony Wood
eBook ISBN: 9780080467412
Paperback ISBN: 9780120405411
Imprint: Academic Press
Published Date: 8th December 2006
Page Count: 556
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Table of Contents



Novel Approaches for the Treatment of Schizophrenia

1 Introduction

2 Approaches targeting altered NMDA receptor function

3 Approaches primarily targeting cognition

4 Approaches primarily targeting psychosis

5 Emerging mechanisms and conclusions

Recent Strategies for the Development of New Antidepressant Drugs

1 Introduction

2 Monoamine reuptake inhibitors

3 SSRIs with monoaminergic receptor modulation

4 Serotonergic receptor modulation

5 Neuropeptide receptor modulation

6 Conclusion

Neuroprotective Agents for the Treatment of Ischemic and Hemorrhagic Stroke

1 Introduction

2 Conclusion

Novel Sodium Channel Blockers for the Treatment of Neuropathic Pain

1 Introduction

2 Background

3 Biological target validation

4 Discovery of novel small molecule blockers

5 Conclusions

Centrally Acting Anti-Obesity Agents

1 Introduction

2 CB1R Antagonists

3 Neuropeptide receptor modulators

4 Aminergic receptor modulators

5 Monoamine re-uptake inhibitors

6 Conclusions

Nuclear Hormone Receptor Modulators for the Treatment of Diabetes and Dyslipidemia

1 Introduction


3 RXR modulators



6 Conclusion

11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors

1 Introduction

2 11β-HSD Isozymes

3 Potential therapeutic indications

4 11β-HSD1 Inhibitors

5 Conclusion

Glucokinase Activators for the Treatment of Type 2 Diabetes

1 Introduction

2 Biology of glucokinase

3 Small-molecule glucokinase activators

4 Conclusion and outlook

Renin Inhibitors

1 Introduction

2 Biology

3 Classical renin inhibitors

4 Aliskiren

5 Piperidines

6 Piperazines

7 Aminopyrimidines

8 Conclusion

Antiarrhythmic Agents

1 Introduction

2 Potassium channel modulators

3 Other antiarrhythmic approaches

4 Miscellaneous approaches

Progress in Anti-SARS Coronavirus Chemistry, Biology and Chemotherapy

1 Introduction

2 SARS coronavirus proteases

3 SARS-CoV 3CLpro inhibitors

4 PLpro inhibitors

5 Viral entry inhibitors

6 Miscellaneous inhibitors

7 Future outlook

Inhibitors of the Expression of Vascular Cell Adhesion Molecule-1

1 Introduction

2 Therapeutic potential

3 Antioxidants

4 Cyclic depsipeptides

5 Chalcones

6 Other compounds

7 Conclusion

Recent Advances in Gastrointestinal Prokinetic Agents

1 Introduction

2 Prokinetic agent target classes

3 Conclusions

PGD2 Antagonists

1 Introduction

2 DP Antagonists

3 CRTH2 Antagonists

4 Conclusion

Progress in the Development of Inhaled, Long-Acting β2-Adrenoceptor Agonists

1 Introduction

2 Quinolinones (8-hydroxycarbostyril)

3 Formamides

4 Saligenins

5 New head groups

6 Dual pharmacology

7 Conclusion

The Acyl Sulfonamide Antiproliferatives and Other Novel Antitumor Agents

1 Introduction

2 The acyl sulfonamide antiproliferatives

3 SNS-595

4 Other novel antiproliferative agents

5 Summary and outlook

Progress on Mitotic Kinesin Inhibitors as Anti-cancer Therapeutics

1 Introduction

2 Inhibitors of kinesin spindle protein

3 Conclusions

Developing Infectious Disease Strategies for the Developing World

1 Introduction

2 Avian influenza


4 Conclusion

Influenza Neuraminidase Inhibitors as Antiviral Agents

1 Introduction

2 Inhibitors based upon six-membered heterocycles

3 Inhibitors based on five-membered ring structures

4 Drugs approved or under clinical trial

5 Conclusions

Recent Developments in Antifungal Drug Discovery

1 Introduction

2 Advances in antifungals with known mechanism of action

3 Emerging antigungal agents

4 Trends in antifungal drug discovery

Genomic Data Mining and Its Impact on Drug Discovery

1 Introduction

2 Gene expression profiling

3 Classification of human cancers using microRNA expression profiles

4 Pharmacogenetics and drug metabolism

5 Conclusion

HTS of cDNA and RNAi for Target Identification

1 Introduction

2 High-throughput reverse genetics screens in cell-based systems

3 Gain of function screens using mammalian cDNAs

Genomic Approaches to Identify Molecular Basis of Multi-Factorial Diseases

1 Introduction

2 The complexities of the human genome

3 Current status of our understanding of human diseases at the molecular level

4 New methods to identify genes and pathways activated in complex multi-factorial diseases

5 Future directions

Structure–Activity Relationships for In vitro and In vivo Toxicity

1 Introduction

2 Structure–toxicity relationships where outcomes may be associated with specific structural fragments

3 Toxicities linked to descriptors for the overall properties of the molecule

4 Predicting structure–toxicity relationships

5 Conclusion

Importance of Early Assessment of Bioactivation in Drug Discovery

1 Introduction

2 Assays to monitor formation of reactive metabolites

3 Strategic directions

The Application of Pulmonary Inhalation Technology to Drug Discovery

1 Introduction

2 The lungs

3 Absorption and bioavailability

4 Pharmacokinetics

5 Safety

6 Inhalation dosage form and delivery system considerations

7 Inhalation product development

8 Inhalation products

9 Conclusions

Recent Advances in Oral Prodrug Discovery

1 Introduction

2 Prodrugs of poorly soluble compounds

3 Prodrugs of polar compounds

4 Prodrugs targeting active transporters

5 Prodrugs for targeted tissue delivery

6 Prodrugs with other benefits

7 Conclusions

Oxytocin Antagonists and Agonists

1 Introduction

2 Oxytocin antagonists

3 Oxytocin agonists

4 Conclusions

Knowledge and Intelligence in Drug Design

1 Introduction

2 Possession of facts

3 Possession of skill

4 Artifical intelligence in drug design

5 Conclusion

To Market, To Market – 2005

1 Introduction

2 Ciclesonide (asthma, COPD)

3 Clofarabine (anticancer)

4 Darifenacin (urinary incontinence)

5 Deferasirox (chronic iron overload)

6 Doripenem (antibiotic)

7 Eberconazole (antifungal)

8 Entecavir (antiviral)

9 Eszopiclone (hypnotic)

10 Exenatide (anti-diabetic)

11 Galsulfase (mucopolysaccharidosis VI)

12 Luliconazole (antifungal)

13 Lumiracoxib (anti-inflammatory)

14 Nepafenac (anti-inflammatory)

15 Pegaptanib (age-related macular degeneration)

16 Pramlintide (anti-diabetic)

17 Palifermin (mucositis)

18 Ramelteon (insomnia)

19 Rasagiline (Parkinson's disease)

20 Sorafenib (anticancer)

21 Tamibarotene (anticancer)

22 Tigecycline (antibiotic)

23 Tipranavir (HIV)

24 Udenafil (erectile dysfunction)

25 Ziconotide (severe chronic pain)

Compound Name, Code Number and Subject Index. Vol. 41

Cumulative Chapter Titles Keyword Index, Vol. 1–41

Cumulative NCE Introduction Index, 1983–2005

Cumulative NCE Introduction Index, 1983–2005 (By Indication)


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. Sections I-IV are disease orientated and generally report on specific medicinal agents. Sections V and VI continue to emphasize important topics in medicinal chemistry, biology, and drug design. Section VII looks at Trends and Perspectives in the pharmaceuticals market.

Key Features

  • Critical reviews of the previous year's literature in many topics of interest to medicinal chemists
  • Highlights major developments in medicinal chemistry
  • Includes a comprehensive set of cumulative indices to easily locate topics in all published volumes


medicinal, pharmaceutical and organic chemists


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© Academic Press 2006
Academic Press
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About the Serial Editors

Anthony Wood Serial Editor

Affiliations and Expertise

Pfizer Global Research and Development, Sandwich Laboratories, Sandwich, Kent, UK