Discussion

From the time they were discovered up until around the turn of the century, macrocycles have been treated as exceptions which eluded the regulations (e.g. Ro5) painstakingly created for a successful drug discovery process. Lately it has become evident that this class of compounds has grown in importance - in particular but not exclusively - in the field of protein-protein interactions.
This hindsight has led to a development boom in the field of the synthesis of macrocyclic substances which however often only partially address the expectations of chemists in preclinical research. We remember the early days of combinatorial chemistry…
This presentation will highlight how substructures from natural compounds can be integrated into the design of macrocycles with improved attractiveness for the medicinal chemist.