Diverse Peptidyl Privileged Structures as Potent Somatostatin Receptor Ligands

This report describes the evaluation of a wide range of structurally diverse “privileged structures”, either amines or acids, linked via urea and amide connections, to the key dipeptide D-Trp-Lys-OMe. This led to the discovery of a collection of potent and structurally distinct SSTR2 ligands in both the amide and urea series. The 4- (benzimidazolone)-piperidine linked SSTR2 agonist (8) is highlighted.