Macrocycles in Drug Discovery

By Jeremy Levin (Editor), David Rotella (Editor), David Newman (Contribution by), Karl Heinz Altmann (Contribution by), A Ganesan (Contribution by), Anders Poulsen (Contribution by), Michael Burnet (Contribution by), Wieslaw Kazmierski (Contribution by), David Fairlie (Contribution by), Daniel Obrecht (Contribution by), Eric Feyfant (Contribution by), Alan Mathiowetz (Contribution by), Mark Peterson (Contribution by)

The medicinal chemistry of natural products is interesting in itself, but lessons learned from these compounds, in terms of the relationship between structure and desirable physicochemical properties, is now informing the design of fully synthetic drug candidates against a variety of targets. Furthermore, as more and more non-classical drug targets, such as protein-protein interactions, are pursued in the pharmaceutical industry, macrocyclic molecules are becoming increasingly important as they offer a way to provide drug-protein interactions that cover a larger surface area than traditional small molecules. An indication of this growing importance is the fact that several companies now provide libraries of macrocyclic molecules produced by proprietary chemical technology to use for lead generation. A variety of macrocyclic natural products have become important drugs or have been identified as leads to marketed drugs.

This book reviews macrocycles in drug discovery, both those of natural origin and semi-synthetic derivatives of natural products, and those designed and synthesized based on principles of medicinal chemistry. Itdiscusses these compounds in the context of their broad chemotype as compounds composed of large rings. Providing a wide reaching review of this important area in a single volume, this book is of interest to biochemists, pharmaceutical scientists and medicinal chemists working in industry or academia."


"The book is a wellmade snapshot of current research, describing development stories of established macrocycle drugs and their properties, as well as new avenues in their development."

"The book s 11 chapters, written by distinguished experts, are mostly dedicated to macrocycles for a specific protein target or target class."

"Numerous examples presented along with the compounds potency, selectivity, permeability, bioavailability and other properties allow the reader to understand which determinants make a successful macrocyclic drug."--Christian Heinis "Chemistry World ""


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About the Hardcover

Publisher Royal Society of Chemistry
Publish date 10/16/2014
Pages 528
ISBN-13 9781849737012
ISBN-10 1849737010
Language English