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Macrocycles are an exceptionally interesting structural class of small molecules with proven therapeutic value that have been the subject of medicinal chemistry research for many years. The increasing effort devoted to the design and synthesis of macrocyclic molecules in both academic and industrial drug discovery programmes, with exciting developments in understanding the determinants of properties such as potency, selectivity, permeability and bioavailability for these molecules, as well as advances in the synthetic methodologies that provide access to them, has provided the impetus for the construction of this volume.

It is the goal of this book to bring together scientific experts, who have been directly involved in research to discover and develop drugs based on macrocyclic scaffolds, and afford them a forum to present the state of the art in their field including, in some cases, drugs with exciting potential that have advanced to clinical trials or to the market. It is my hope that the topics covered herein will provide essential background information on the genesis and evolution of macrocyclic compounds in drug discovery, as well as offering a sense of the promise of what this field may deliver in the future.

I would like to express my great appreciation to each of the chapter authors for the time and effort spent to write informative reviews on their respective areas of research. I would also like to express my appreciation to Professor David Rotella (Montclair State University), and Rosalind Searle, Helen Prasad and Rowan Frame at the Royal Society of Chemistry for their help, support and patience in the course of putting together this book.

Jeremy I. Levin

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