High-Throughput Lead Optimization in Drug Discovery

ISBN-13: 9780367387716 / Angielski / Miękka / 2019 / 256 str.

Tushar Kshirsagar

Opis

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.

Spis treści

Introduction and Review. Application of Parallel Synthesis to the Optimization of Inhibitors of the ZipA-FtsZ Protein-Protein Interaction. Case Studies of Parallel Synthesis in Hit Identification, Hit Exploration, Hit-to-Lead, and Lead Optimization Programs. A Successful Application of Parallel Synthesis to Computer-Assisted Structural Optimization of New Leads Targeting Human Immunodeficiency Virus-1 Reverse Transcriptase: The Case of Acylthiocarbamates and Thiocarbamates. How High-Throughput Medicinal Chemistry Can Expedite Lead Discovery, Lead Optimization, and Beyond. Rapid Lead Identification of Inhibitors of Adenine Nucleotide Translocase: A Case Study of Applying Combinatorial Chemistry Techniques in Drug Discovery. Parallel Synthesis of Anticancer, Antiinflammatory, and Antiviral Agents Derived from L-and D-Amino Acids. Application of Solid-Phase Parallel Synthesis in Lead Optimization Studies. High-Throughput Solid-Phase Synthesis of Nucleoside-Based Libraries in the Search for New Antibiotics.

O autorze

Tushar Kshirsagar