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

Affiliation

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.

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