Including case studies of macrocyclic marketed drugs and macrocycles in drug development, this book helps medicinal chemists deal with the synthetic and conceptual challenges of macrocycles in drug discovery efforts. Provides needed background to build a program in macrocycle drug discovery –design criteria, macrocycle profiles, applications, and limitations Features chapters contributed from leading international figures involved in macrocyclic drug discovery efforts Covers design criteria, typical profile of current macrocycles, applications, and limitations

This volume explores the latest techniques and strategies used to study the field of peptide macrocycles. The chapters in this book ae organized into four parts: macrocycles synthesis, combinational library synthesis and screening, macrocycle characterization, and unique applications. Part One looks at a variety of peptide cyclization methodologies, and Part Two describes methods for the creation of peptide macrocycles libraries and their subsequent screening against biological targets of interest. Part Three discusses the study and characterization of peptide macrocycle-target interactions, and Part Four introduces unique applications for peptide macrocycles, from higher-order structure formation to post-synthetic functional modifications. Written in the highly successful Methods in Molecular Biology series format, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and tips on troubleshooting and avoiding known pitfalls. Cutting-edge and comprehensive, Peptide Macrocycles: Methods and Protocols is a valuable resource for both novice and expert researchers looking to learn more about this developing field.

This series provides a comprehensive resource for postgraduate students and for scientists in academia or industry wanting to learn topics outside their own areas of expertise.

This book provides a complete overview of cucurbituril chemistry, covering fundamental aspects including history, synthesis and host-guest chemistry.

The Chemistry of Heterocyclic Compounds, since its inception, has been recognized as a cornerstone of heterocyclic chemistry. Each volume attempts to discuss all aspects – properties, synthesis, reactions, physiological and industrial significance – of a specific ring system. To keep the series up-to-date, supplementary volumes covering the recent literature on each individual ring system have been published. Many ring systems (such as pyridines and oxazoles) are treated in distinct books, each consisting of separate volumes or parts dealing with different individual topics. With all authors are recognized authorities, the Chemistry of Heterocyclic Chemistry is considered worldwide as the indispensable resource for organic, bioorganic, and medicinal chemists.

Stereochemical and Stereophysical Behavior of Macrocycles deals with the stereochemical and stereophysical properties of macrocyclic ligands and their coordination compounds. More specifically, the stereochemistry of metallic macrocyclics is discussed, along with the relationship between the thermodynamics and stereochemistry of macrocyclics and cryptates. The stereochemical aspects of the macrocycles of second and third row transition elements are also examined. Comprised of three chapters, this volume begins with an introduction to the stereochemistry of metallic macrocyclics as well as their structure, together with the conformation of their chemical rings and the steric effects of their coordination geometry. The next chapter considers the relationship between the thermodynamics and stereochemistry of macrocyclics and cryptates, with particular reference to the macrocyclic and cryptate effect. Cation-ligand interactions and solvent effects upon complex formation are described, along with macrocyclic and macrobicyclic ligands having different donor atoms. The final chapter is devoted to the stereochemical aspects of the macrocycles of transition metal ions, with additional comments on the stereochemistry of copper and nickel in unusual oxidation states. This book will be of interest to inorganic chemists.

Including case studies of macrocyclic marketed drugs and macrocycles in drug development, this book helps medicinal chemists deal with the synthetic and conceptual challenges of macrocycles in drug discovery efforts. Provides needed background to build a program in macrocycle drug discovery –design criteria, macrocycle profiles, applications, and limitations Features chapters contributed from leading international figures involved in macrocyclic drug discovery efforts Covers design criteria, typical profile of current macrocycles, applications, and limitations