Chapter 10 - Macrocycles: Under-Explored and Poorly Exploited Drug Class Despite the Proven Therapeutic Potential

Abstract

Because macrocyclic ring structures cover a unique chemical space, they represent an opportunity to unlock novel targets that are difficult to address with classical small molecules. Indeed, macrocyclic derivatives have unique physicochemical properties. In the past, all macrocyclic drugs originated from natural products. Recent success stories reported with synthetic macrocycles coupled with the growing capacity to generate these molecules using novel macrocyclization procedures have encouraged scientists to enter this largely unexplored field of medicinal chemistry and extend their collection of larger molecule libraries. It is therefore likely that the macrocycles will deliver attractive new drugs addressing important unmet medical needs.