Chapter Twenty-Three – Synthetic Macrocycles in Small-Molecule Drug Discovery

Abstract Macrocycles are receiving increased attention in small-molecule drug discovery, due, at least in part, to the impact of macrocyclization on novel chemical space, new protein targets for drug discovery and PK/PD properties, as well as advances in macrocycle synthesis. We review several current drug discovery targets for which synthetic macrocycles have advanced drug discovery efforts, and we briefly discuss some issues related to understanding the impact of macrocyclization on small-molecule drug properties.