Preface

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

It is the goal of this book to bring together scientific experts, who havebeen directly involved in research to discover and develop drugs based onmacrocyclic scaffolds, and afford them a forum to present the state of the artin their field including, in some cases, drugs with exciting potential thathave advanced to clinical trials or to the market. It is my hope that the topicscovered herein will provide essential background information on the genesisand evolution of macrocyclic compounds in drug discovery, as well asoffering 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 chapterauthors for the time and effort spent to write informative reviews on theirrespective areas of research. I would also like to express my appreciation toProfessor David Rotella (Montclair State University), and Rosalind Searle,Helen Prasad and Rowan Frame at the Royal Society of Chemistry for theirhelp, support and patience in the course of putting together this book.

Jeremy I. Levin

RSC Drug Discovery Series No. 40Macrocycles in Drug DiscoveryEdited by Jeremy Levinr The Royal Society of Chemistry 2015Published by the Royal Society of Chemistry, www.rsc.org

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