Traditionally, the search for new compounds from natural products has been a time- and resource-intensive process. The recent application of combinatorial methods and high-throughput synthesis has allowed scientists to generate a range of new molecular structures from natural products and observe how they interact with biological targets. Combinatorial Synthesis of Natural Product-Based Libraries summarizes the most important perspectives on the application of combinatorial chemistry and natural products to novel drug discovery.

The book details the latest approaches for implementing combinatorial research and testing methodologies to the synthesis of natural product-based libraries. Interconnecting the important aspects of this emerging field through the work of several leading scientists, it covers the computational analysis of natural molecules and details strategies for designing compound libraries, using bioinformatics in particular. The authors describe numerous synthetic methods for producing natural products and their analogs, including engineered biosynthesis and polymer-supported reagents. They also discuss additional considerations for generating libraries, such as screening, scaffolding, and yield optimization. Other chapters examine specific classes of libraries derived from natural products including carbohydrates, polyketides, peptides, alkaloids, terpenoids, steroids, flavonoids, and fungal compounds.

Drawing attention to the interplay of drug discovery, natural products, and organic synthesis, Combinatorial Synthesis of Natural Product-Based Libraries contains the most recent and significant methods used to search and assess new compounds for their ability to mitigate biological processes that may lead to improved treatments for various diseases.

Combinatorial Synthesis of Natural Product-Based Libraries presents the latest approaches in the implementation of combinatorial research methodologies for the synthesis of natural product-based libraries. It describes strategies and designs for successful synthesis, summarizing the challenges and opportunities in the combinatorial organic synthesis of natural product-based libraries. It also examines how to improve efficiency of combinatorial screening by using natural products in the design of screening compounds. Highlighting new developments in synthetic, organic, and combinatorial chemistry, this text serves combinatorial and medicinal chemists as well as natural products scientists.

"[This book] elegantly reviews recent efforts to develop high-diversity compound libraries based on natural products. ...From the historical developments to the latest technologies, from the identification of a suitable target to the building of the library, every step is documented and highlighted by many examples. ...A huge amount of references give the readers the opportunity to return to the original papers... ... A large amount of appealing Figures and Schemes illustrate the concepts discussed in the text. The Chapters are well structured... As the authors are from different backgrounds, the book covers various strategies, various synthetic methods, and all types of compound families. ...[A] valuable tool for everybody working in medicinal chemistry as well as the agrochemical, industrial, or academic domains.
- François Diederich, Swiss Federal Institute of Technology, Zurich

"...Elegantly reviews recent efforts to develop high-diversity compound libraries based on natural products. ...From the identification of a suitable target to the building of the library, every step is documented and highlighted by many examples. ..."
- François Diederich, Swiss Federal Institute of Technology, Zurich

"A first-rate source of information to learn about different planning strategies"
-Victor E. Marquez in Journal of Medicinal Chemistry 2007, Vol. 50, No. 5 (2007)