Princeton chemists report rhodium-catalysed route to macrocyclic antibiotic peptides

The wire

1. 01Princeton researchers describe a rhodium-catalysed macrocyclization using a dual-functional directing group to make tryptophan-crosslinked macrocyclic peptides, including tryglysin pharmacophores.
2. 02Macrocyclic peptide chemistry underpins the oral and constrained-peptide pipeline readers track, where synthetic access is a persistent bottleneck.
3. 03This is synthetic methodology only; no antibacterial potency, pharmacokinetic or in vivo data are reported in the summary.

From the source

Chemists Crack the Recipe for Ring-Shaped Antibiotic Peptides with a Two-Job Molecular Handle

Princeton chemists have developed a rhodium-catalysed macrocyclization using a dual-functional directing group that enables general synthesis of tryptophan-crosslinked macrocyclic peptides, including pharmacophores of the antibiotic tryglysin.