Progress in Medicinal Chemistry, Volume 56 provides a review of eclectic developments in medicinal chemistry. This volume includes chapters covering recent advances in cancer therapeutics, fluorine in medicinal chemistry, a perspective on the next generation of antibacterial agents derived by manipulation of natural products, a potential new era for Chagas Disease drug discovery, and imaging in drug development. Specific chapters cover timely topics, such as the development of LRRK2 inhibitors for the treatment of Parkinson's, and recent discoveries and developments in TRPA1 modulators.
Users will find a comprehensive resource on the topic of medicinal chemistry that also discusses avenues for the acceleration of drug discovery programs.
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Contains eclectic developments in medicinal chemistry, with authoritative extended reviews of targets and technologies addressing new therapeutics
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vii | |
| Preface |
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ix | |
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1 Enabling Chemistry Technologies and Parallel Synthesis---Accelerators of Drug Discovery Programmes |
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1 | (36) |
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2 The Evolution of Flow-Based Approaches to Synthesis |
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3 | (1) |
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3 Use of High-Temperature Chemistries |
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3 | (4) |
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4 Use of Photochemical and Electrochemical Reactions |
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7 | (6) |
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5 Use of Hazardous Gases (e.g. Diazomethane) in Flow |
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13 | (4) |
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6 Library Design Tools and Processes |
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17 | (8) |
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7 Use of Flow Chemistry for Library Synthesis |
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25 | (5) |
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8 Summary and Future Perspectives |
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30 | (7) |
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31 | (1) |
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31 | (6) |
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2 Development of LRRK2 Inhibitors for the Treatment of Parkinson's Disease |
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37 | (44) |
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37 | (1) |
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38 | (5) |
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3 Structural Biology of LRRK2 |
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43 | (2) |
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4 Overview of Selective Inhibitors of LRRK2 |
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45 | (26) |
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71 | (10) |
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73 | (8) |
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3 Recent Progress in the Discovery and Development of TRPA1 Modulators |
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81 | (36) |
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81 | (3) |
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2 Validation as a Target for Drug Discovery |
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84 | (7) |
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3 Medicinal Chemistry and Clinical Status of TRPA1 Modulators |
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91 | (13) |
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4 Recent Structural Insights |
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104 | (1) |
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5 Conclusions and Outlook |
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105 | (12) |
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106 | (11) |
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4 Small Molecule Inhibition of Interleukin-1 Receptor-Associated Kinase 4 (IRAK4) |
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117 | (48) |
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118 | (7) |
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2 Small Molecule IRAK4 Inhibitor Discovery |
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125 | (30) |
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3 Summary of Clinical Status |
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155 | (1) |
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156 | (9) |
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156 | (9) |
| Index |
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165 | (4) |
| Cumulative Index of Authors |
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169 | (8) |
| Cumulative Index of Subject |
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177 | |
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. Professor Brian Cox is at University of Sussex, Brighton, UK
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