Synthesis and pharmacological characterization of 5-phenyl-2-[2-(1-piperidinylcarbonyl)phenyl]-2,3-dihydro-1H-pyrrolo[1,2-c]imidazol-1-ones: a new class of Neuropeptide S antagonists

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7308-11. doi: 10.1016/j.bmcl.2010.10.067. Epub 2010 Oct 21.

Abstract

A new class of selective NPS antagonist was developed starting from a commercially available product identified by screening activities. Experimental NMR observations and computational experiments allowed the discovery of a new class of derivatives. 5-Phenyl-2-[2-(1-piperidinylcarbonyl)phenyl]-2,3-dihydro-1H-pyrrolo[1,2-c]imidazol-1-one represents a new lead compound in the NPS antagonist field.

MeSH terms

  • Animals
  • Azabicyclo Compounds / chemistry*
  • Computer Simulation
  • Drug Design
  • Humans
  • Imidazoles / chemical synthesis
  • Imidazoles / chemistry*
  • Imidazoles / pharmacology
  • Microsomes, Liver / metabolism
  • Neuropeptides / antagonists & inhibitors*
  • Neuropeptides / metabolism
  • Piperidines / chemistry*
  • Rats
  • Thermodynamics

Substances

  • Azabicyclo Compounds
  • Imidazoles
  • Neuropeptides
  • Piperidines
  • neuropeptide S, human