Bioorganic & Medicinal Chemistry Letters 2004-05-03

Indoline derivatives as 5-HT(2C) receptor agonists.

J M Bentley, D R Adams, D Bebbington, K R Benwell, M J Bickerdike, J E P Davidson, C E Dawson, C T Dourish, M A J Duncton, S Gaur, A R George, P R Giles, R J Hamlyn, G A Kennett, A R Knight, C S Malcolm, H L Mansell, A Misra, N J T Monck, R M Pratt, K Quirk, J R A Roffey, S P Vickers, I A Cliffe

Index: Bioorg. Med. Chem. Lett. 14 , 2367-2370, (2004)

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Abstract

A series of 1-(1-indolinyl)-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 all of the compounds at 5-HT(2) receptor subtypes are reported. A number of compounds were found to reduce food intake in rats after oral administration.