Identification of small molecule agonists of the motilin receptor

Bioorg Med Chem Lett. 2008 Dec 15;18(24):6423-8. doi: 10.1016/j.bmcl.2008.10.071. Epub 2008 Oct 19.

Abstract

High-throughput screening resulted in the identification of a series of novel motilin receptor agonists with relatively low molecular weights. The series originated from an array of biphenyl derivatives designed to target 7-transmembrane (7-TM) receptors. Further investigation of the structure-activity relationship within the series resulted in the identification of compound (22) as a potent and selective agonist at the motilin receptor.

MeSH terms

  • Animals
  • Binding Sites
  • Cell Membrane / metabolism
  • Chemistry, Pharmaceutical / methods
  • Combinatorial Chemistry Techniques
  • Drug Design
  • Drug Evaluation, Preclinical
  • Humans
  • Models, Chemical
  • Molecular Structure
  • Receptors, G-Protein-Coupled / metabolism
  • Receptors, Gastrointestinal Hormone / agonists*
  • Receptors, Gastrointestinal Hormone / chemistry*
  • Receptors, Neuropeptide / agonists*
  • Receptors, Neuropeptide / chemistry*
  • Recombinant Proteins / chemistry
  • Structure-Activity Relationship

Substances

  • Receptors, G-Protein-Coupled
  • Receptors, Gastrointestinal Hormone
  • Receptors, Neuropeptide
  • Recombinant Proteins
  • motilin receptor