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

  • Bioorg Med Chem Lett. 2006 Feb;16(3):677-80. doi: 10.1016/j.bmcl.2005.10.029.
David R Adams  1 ,  Jonathan M Bentley ,  Karen R Benwell ,  Michael J Bickerdike ,  Corinna D Bodkin ,  Ian A Cliffe ,  Colin T Dourish ,  Ashley R George ,  Guy A Kennett ,  Antony R Knight ,  Craig S Malcolm ,  Howard L Mansell ,  Anil Misra ,  Kathleen Quirk ,  Jonathan R A Roffey ,  Steven P Vickers
Affiliations
  • 1. Vernalis plc, Oakdene Court, 613 Reading Road, Winnersh, Wokingham, Berkshire RG41 5UA, UK.
PMID: 16257207 DOI: 10.1016/j.bmcl.2005.10.029
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.