Pyrrolo(iso)quinoline derivatives as 5-HT2C receptor agonists

A series of 1-(1-pyrrolo(iso)quinolinyl)-2-propylamines was synthesised and evaluated as 5-HT2C 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-HT2 receptor subtypes are reported. The analogue which showed the highest 5-HT2C binding affinity (27, 1.6 nM) was found to be successful in reducing food intake in rats.

A series of 1-(1-pyrrolo(iso)quinolinyl)-2-propylamines was prepared and evaluated as 5-HT2C receptor agonists for the treatment of obesity.Figure optionsDownload as PowerPoint slide