Normalization of excessive glutamate neurotransmission through activation of the metabotropic glutamate receptor 2 (mGluR2) represents a novel approach for the treatment of schizophrenia. Clinical validation of this approach was achieved in a Phase II study in schizophrenic patients with orthosteric mGluR2/3 agonist LY404039. Alternatively, positive allosteric modulators (potentiators) of mGluR2 may offer advantages over orthosteric mGluR2/3 agonists as a result of their unique mode of action and selectivity. Herein we describe the lead optimization of oxazolidinone (1) into oxazolobenzimidazole (2). 

Development of an oxazolobenzimidazole class of positive allosteric modulators of mGluR2 for the treatment of schizophrenia

240th National Meeting (2010)

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