High-Throughput Lead Optimization in Drug Discovery

A single source on parallel synthesis for lead optimization, this book features real-world examples and contributions from well-known scientists. It explores the shift to conducting parallel lead optimization in-house while outsourcing most of the screening libraries synthesis. With 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 authors explain the design principles they used to direct the choice of templates and diversity elements and they explore how this technology, when applied to library design, can speed up drug discovery.