A DIVERSITY-ORIENTED SYNTHESIS OF MACROCYCLIC PEPTIDOMIMETICS WITH UNPRECEDENTED SCAFFOLD DIVERSITY

Macrocycles (ring structures of 12 or more atoms) are important core scaffolds that contribute significantly to the overall 3D conformation of molecules and thus how they present chemical information.1 Macrocyclic peptidomimetics are a subclass of macrocycles that are designed to act as functional substitutes of peptide motifs or proteins, displaying more desirable properties such as improved metabolic and proteolytic stability.2 Despite their useful properties, macrocyclic peptidomimetics represent an underexplored structural class within drug discovery. This is often attributed to the lack of general synthetic methods for producing collections o