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

Bioorg Med Chem Lett. 2007 Aug 1;17(15):4187-90. doi: 10.1016/j.bmcl.2007.05.043. Epub 2007 May 18.

Abstract

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.

MeSH terms

  • Amino Acids / chemistry*
  • Cyclization
  • Macrocyclic Compounds / pharmacology*
  • Receptors, Gastrointestinal Hormone / antagonists & inhibitors*
  • Receptors, Gastrointestinal Hormone / chemistry
  • Receptors, Neuropeptide / antagonists & inhibitors*
  • Receptors, Neuropeptide / chemistry

Substances

  • Amino Acids
  • Macrocyclic Compounds
  • Receptors, Gastrointestinal Hormone
  • Receptors, Neuropeptide
  • motilin receptor