High-throughput Lead Optimization in Drug Discovery

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  • Edition: 1st
  • Format: Hardcover
  • Copyright: 2008-03-04
  • Publisher: CRC Press

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A Single Source on Parallel Synthesis for Lead OptimizationThe end of the previous millennium saw an explosion in the application of parallel synthesis techniques for making compounds for high-throughput screening. Over time, it became clear that more thought in the design phase of library development is necessary to generate high quality hits. More recently, the use of parallel synthesis techniques has shifted to applications beyond screening collections. Exploring the nuances of this technology, High-Throughput Lead Optimization in Drug Discoverydescribes the application of parallel synthesis to lead optimization and the design and synthesis of targeted libraries. Examine Case Studies that Cover a Range of Different Biological TargetsFeaturing real-world examples and contributions from well-known scientists, the book explores the shift to conducting parallel lead optimization in-house while outsourcing most of the screening librariessynthesis. It includes more than 15 case studies that encompass a range of biological targets for application in different therapeutic areas. The text contains examples of solid and solution-phase techniques for the synthesis of directed libraries. The chapter authors explain the design principles they used to direct the choice of templates and diversity elements. Speed Up Drug Discovery and the Hit-to-Lead ProcessFocusing on the application of combinatorial chemistry to medicinal chemistry, this volume compiles a series of optimization projects that give you a snapshot of successes and challenges in the use of parallel synthesis for lead optimization. It explores how this technology, when applied to library design, can speed up drug discovery.

Table of Contents

Introduction and Reviewp. 1
Application of Parallel Synthesis to the Optimization of Inhibitors of the ZipA-FtsZ Protein-Protein Interactionp. 85
Case Studies of Parallel Synthesis in Hit Identification, Hit Exploration, Hit-to-Lead, and Lead Optimization Programsp. 99
A Successful Application of Parallel Synthesis to Computer-Assisted Structural Optimization of New Leads Targeting Human Immunodeficiency Virus-I Reverse Transcriptase: The Case of Acylthiocarbamates and Thiocarbamatesp. 117
How High-Throughput Medicinal Chemistry Can Expedite Lead Discovery, Lead Optimization, and Beyondp. 151
Rapid Lead Identification of Inhibitors of Adenine Nucleotide Translocase: A Case Study of Applying Combinatorial Chemistry Techniques in Drug Discoveryp. 165
Parallel Synthesis of Anticancer, Antiinflammatory, and Antiviral Agents Derived from L- and D-Amino Acidsp. 177
Application of Solid-Phase Parallel Synthesis in Lead Optimization Studiesp. 195
High-Throughput Solid-Phase Synthesis of Nucleoside-Based Libraries in the Search for New Antibioticsp. 215
Indexp. 239
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