Novel pyrazolopiperazinone- and pyrrolopiperazinone-based MCH-R1 antagonists

Bioorg Med Chem Lett. 2007 Feb 1;17(3):657-61. doi: 10.1016/j.bmcl.2006.10.096. Epub 2006 Nov 6.

Abstract

The synthesis and biological testing of novel classes of potent melanin-concentrating hormone (MCH-R1) antagonists based on pyrazolopiperazinone and pyrrolopiperazinone scaffolds are described.

MeSH terms

  • Caco-2 Cells
  • Humans
  • Indicators and Reagents
  • Models, Molecular
  • Molecular Conformation
  • Piperazines / chemical synthesis*
  • Piperazines / pharmacology
  • Pyrazoles / chemical synthesis*
  • Pyrazoles / pharmacology
  • Pyrroles / chemical synthesis*
  • Pyrroles / pharmacology
  • Radioligand Assay
  • Receptor, Serotonin, 5-HT2C / drug effects
  • Receptors, Somatostatin / antagonists & inhibitors*

Substances

  • Indicators and Reagents
  • MCHR1 protein, human
  • Piperazines
  • Pyrazoles
  • Pyrroles
  • Receptor, Serotonin, 5-HT2C
  • Receptors, Somatostatin
  • pyrazolopiperazinone
  • pyrrolopiperazinone