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Bioorganic and Medicinal Chemistry Letters 2006-Feb

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

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David R Adams
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

Keywords

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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