Studies towards the identification of a new generation of atypical antipsychotic agents

…, IT Forbes, AD Gribble, MS Hadley, AP Lightfoot…

Index: Garzya, Vincenzo; Forbes, Ian T.; Gribble, Andrew D.; Hadley, Mike S.; Lightfoot, Andrew P.; Payne, Andrew H.; Smith, Alexander B.; Douglas, Sara E.; Cooper, David G.; Stansfield, Ian G.; Meeson, Malcom; Dodds, Emma E.; Jones, Declan N.C.; Wood, Martyn; Reavill, Charlie; Scorer, Carol A.; Worby, Angela; Riley, Graham; Eddershaw, Peter; Ioannou, Chris; Donati, Daniele; Hagan, Jim J.; Ratti, Emiliangelo A. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 2 p. 400 - 405

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Citation Number: 51

Abstract

A rational structure–activity relationship study around compound (1) is reported. The lead optimisation programme led to the identification of sulfonamide (25), a molecule combining dopamine D2/D3 receptor antagonism with serotonin 5-HT2A, 5-HT2C, 5-HT6 receptor antagonism for an effective treatment of schizophrenia. Compound (25) was shown to possess the required in vivo activity with no EPS liability.