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

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, which possess great potential for difficult therapeutic targets. Because of this, there is now extensive interest in the use of macrocycles for drug discovery and raises the need for a handy guidebook about the basics and practices of working with them.

Including case studies of macrocyclic marketed drugs and macrocycles in drug development, A Medicinal Chemist′s Guide to 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, synthetic methods to make macrocycles, and case studies of macrocyclic marketed drugs and macrocycles in drug development.

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

          Needed background to build a program in macrocycle drug discovery design criteria, macrocycle profiles, applications, and limitations

          Help to deal with the synthetic and conceptual challenges of macrocycles in drug discovery efforts

          Coverage of design criteria, typical profile of current macrocycles, applications, and limitations

Eric Marsault, PhD, is an Associate Professor of pharmacology at the University of Sherbrooke as well as the Director of the Quebec Network for Drug Discovery. Previously, he was 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 25 years of experience in the pharmaceutical industry.