Christian Bisang

A template for the solid-phase synthesis of conformationally restricted protein loop mimetics

A trifunctional template 1 is synthesized from trans-4-hydroxy-L-proline and L-aspartic acid, immobilized on a solid-support, and used for the solid-phase synthesis of a cyclic conformationally restrained hexapeptide loop mimetic containing the motif Asn-Pro-Asn-Ala (NPNA); this is shown by NMR to populate a stable β-turn conformation in aqueous solution.

Advances in macrocyclic peptide-based antibiotics

Macrocyclic peptide-based natural products have provided powerful new antibiotic drugs, drug candidates, and scaffolds for medicinal chemists as a source of inspiration to design novel antibiotics. While most of those natural products are active mainly against Gram-positive pathogens, novel macrocyclic peptide-based compounds have recently been described, which exhibit potent and specific activity against some of the most problematic Gram-negative ESKAPE pathogens. This mini-review gives an up-date on recent developments.