Potent macrocyclic antagonists to the motilin receptor presenting novel unnatural amino acids

Novel, potent small molecule motilin receptor antagonists are described. These peptidomimetic macrocycles are composed of a tripeptide cyclized backbone-to-backbone with a nonpeptidic tether and bear new unnatural amino acids containing basic side chains.

Graphical abstractNew macrocylic peptidomimetics bearing novel unnatural amino acids are reported as potent motilin antagonist.Figure optionsDownload full-size imageDownload as PowerPoint slide