Diversity-Oriented Synthesis: Basics and Applications in Organic Synthesis, Drug Discovery, and Chemical Biology

Discover an enhanced synthetic approach to developing and screening chemical compound libraries

Diversity-oriented synthesis is a new paradigm for developing large collections of structurally diverse small molecules as probes to investigate biological pathways. This book presents the most effective methods in diversity-oriented synthesis for creating small molecule collections. It offers tested and proven strategies for developing diversity-oriented synthetic libraries and screening methods for identifying ligands. Lastly, it explores some promising new applications based on diversity-oriented synthesis that have the potential to dramatically advance studies in drug discovery and chemical biology.

Diversity-Oriented Synthesis begins with an introductory chapter that explores the basics, including a discussion of the relationship between diversity-oriented synthesis and classic combinatorial chemistry. Divided into four parts, the book:

• Offers key chemical methods for the generation of small molecules using diversity-oriented principles, including peptidomimetics and macrocycles
• Expands on the concept of diversity-oriented synthesis by describing chemical libraries
• Provides modern approaches to screening diversity-oriented synthetic libraries, including high-throughput and high-content screening, small molecule microarrays, and smart screening assays
• Presents the applications of diversity-oriented synthetic libraries and small molecules in drug discovery and chemical biology, reporting the results of key studies and forecasting the role of diversity-oriented synthesis in future biomedical research

This book has been written and edited by leading international experts in organic synthesis and its applications. Their contributions are based on a thorough review of the current literature as well as their own firsthand experience developing synthetic methods and applications.

Clearly written and extensively referenced, Diversity-Oriented Synthesis introduces novices to this highly promising field of research and serves as a springboard for experts to advance their own research studies and develop new applications.

Diversity-Oriented Synthesis: Basics and Applications in Organic Synthesis, Drug Discovery, and Chemical Biology
Andrea Trabocchi
Foreword by Stuart L. Schreiber

This book reviews diversity-oriented synthesis (DOS), a leading and dynamic area in organic chemistry and drug discovery. It first covers key chemical methods for the generation of small molecules according to DOS principles as well as important classes of molecules generated through DOS approaches. The concept of diversity-oriented synthesis is then expanded to the description of chemical libraries. The book also examines modern approaches for screening DOS libraries and concludes with significant applications of DOS libraries and small molecules in the fields of drug discovery and chemical biology.