Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists. Article

Adams, David R, Bentley, Jonathan M, Benwell, Karen R et al. (2006). Pyrrolo(iso)quinoline derivatives as 5-HT(2C) receptor agonists. . BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 16(3), 677-680. 10.1016/j.bmcl.2005.10.029

cited authors

  • Adams, David R; Bentley, Jonathan M; Benwell, Karen R; Bickerdike, Michael J; Bodkin, Corinna D; Cliffe, Ian A; Dourish, Colin T; George, Ashley R; Kennett, Guy A; Knight, Antony R; Malcolm, Craig S; Mansell, Howard L; Misra, Anil; Quirk, Kathleen; Roffey, Jonathan RA; Vickers, Steven P

authors

abstract

  • A series of 1-(1-pyrrolo(iso)quinolinyl)-2-propylamines was synthesised and evaluated as 5-HT(2C) receptor agonists for the treatment of obesity. The general methods of synthesis of the precursor indoles are described. The functional efficacy and radioligand binding data for the compounds at 5-HT(2) receptor subtypes are reported. The analogue which showed the highest 5-HT(2C) binding affinity (27, 1.6nM) was found to be successful in reducing food intake in rats.

publication date

  • February 1, 2006

keywords

  • Animals
  • Anti-Obesity Agents
  • Disease Models, Animal
  • Eating
  • Isoquinolines
  • Pyrroles
  • Quinolines
  • Radioligand Assay
  • Rats
  • Serotonin 5-HT2 Receptor Agonists
  • Serotonin Receptor Agonists

Location

  • England

Digital Object Identifier (DOI)

start page

  • 677

end page

  • 680

volume

  • 16

issue

  • 3