Practical Medicinal Chemistry with Macrocycles: Design, Synthesis, and Case Studies 1st Edition

Macrocycles are medium to large ring compounds that offer medicinal chemists the benefits of both small molecules and biomolecules – oral bioavailability and extended surface areas, respectively; as a result, they possess great potential for modulation of difficult therapeutic targets. Accordingly, there is now extensive interest in the use of macrocycles for drug discovery, hence the need for a handy guidebook about the basics and practices of working with such compounds.

Practical Medicinal Chemistry with Macrocycles offers a practical resource for those scientists developing new therapeutic agents. With chapters contributed from leading international figures involved in macrocyclic drug discovery efforts, the book is broken into four parts: challenges specific to macrocycles, classes of macrocycles and their potential in drug discovery, the synthetic toolbox for macrocycles, and case studies of macrocyclic marketed drugs and clinical candidates.

These aspects of the book combine to offer a number of key features that include:

• Background to build a drug discovery program based on macrocycles – design criteria, molecular profiles, applications, potential pitfalls and limitations
• Numerous synthetic approaches and strategies to build, diversify and optimize macrocycles in the context of medicinal chemistry efforts
• A wealth of successful examples and case studies to help deal with the synthetic and conceptual challenges of working with macrocycles

Eric Marsault, PhD, is Professor of Pharmacology and Medicinal Chemistry at the University of Sherbrooke as well as the Director of the Institut de Pharmacologie de Sherbrooke. Previously, he was Group Leader, then Director of Medicinal Chemistry at Tranzyme Pharma, where he worked for eight years.

Mark L. Peterson, PhD, is Chief Operating Officer and Corporate Secretary at Cyclenium Pharma, of which he is a member of the founding management / scientific team. He has over 25 years of experience in the biotechnology and pharmaceutical industries.

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