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Informationen zum Autor Werngard Czechtizky is the Head of Medicinal Chemistry of the German Hub of Sanofi, based in Frankfurt, Germany. She has wide experience in lead generation and lead optimization for central nervous system, cardiovascular and diabetes targets, and her teams have been responsible for a number of leads and clinical candidates in these areas over the last years. She was educated at ETH Zürich and Harvard University, USA. Peter Hamley is the global head of External Innovation and Sourcing for chemistry, computational chemistry, and screening technologies at Sanofi, based in Frankfurt, Germany. He spent ten years at AstraZeneca in the United Kingdom, and then moved to Sanofi as a medicinal chemistry leader, building their automated chemistry capabilities and natural product technology. He was educated at Imperial College, London, the University of Cambridge and the University of Pennsylvania. Klappentext Stressing strategic and technological solutions to medicinal chemistry challenges, this book presents methods and practices for optimizing the chemical aspects of drug discovery. Chapters discuss benefits, challenges, case studies, and industry perspectives for improving drug discovery programs with respect to quality and costs.* Focuses on small molecules and their critical role in medicinal chemistry, reviewing chemical and economic advantages, challenges, and trends in the field from industry perspectives* Discusses novel approaches and key topics, like screening collection enhancement, risk sharing, HTS triage, new lead finding approaches, diversity-oriented synthesis, peptidomimetics, natural products, and high throughput medicinal chemistry approaches* Explains how to reduce design-make-test cycle times by integrating medicinal chemistry, physical chemistry, and ADME profiling techniques* Includes descriptive case studies, examples, and applications to illustrate new technologies and provide step-by-step explanations to enable them in a laboratory setting Zusammenfassung Stressing strategic and technological solutions to medicinal chemistry challenges, this book presents methods and practices for optimizing the chemical aspects of drug discovery. It provides an overview of the field, with a focus on recent trends, up-to-date technologies, and the identification and development of small molecule drugs. Inhaltsverzeichnis List of Contributors xiii Introduction 1 Werngard Czechtizky and Peter Hamley Part I Exploring Biological Space: Access to New Collections 11 1 Elements for the Development of Strategies for Compound Library Enhancement 13 Edgar Jacoby 1.1 Introduction 13 1.2 Chemical Space for Drug Discovery 14 1.3 Molecular Properties for Drug Discovery 17 1.4 Major Compound Classes 21 1.5 Chemical Design Approaches to Expand Bioactive Chemical Space 25 1.6 Conclusion 28 Acknowledgments 29 References 29 2 The European Lead Factory 37 Christopher Kallus, Jörg Hüser, Philip S. Jones, and Adam Nelson 2.1 Introduction 37 2.1.1 Background 37 2.1.2 The European Lead Factory 38 2.2 Building the Joint European Compound Library 43 2.2.1 Definition of Criteria and an Approach for the Review and Selection of Library Proposals 46 2.2.2 Collation, Review, and Selection of an Initial Wave of Library Proposals 47 2.2.3 A Web?]Based Tool to Support the Collation, Review, and Selection of Proposals 49 2.2.4 Synthetic Validation of Library Proposals and Library Production 49 2.3 Qualified Hit Generation 54 2.3.1 Capabilities of the ESC 54 2.3.2 Target Selection and Generation of Qualified Hits 56 2.3.3 Exploitation of Qualified Hit List 58 2.4 Future Perspectives 58 Acknowledgments 59 References 59 ...
