European Journal of Medicinal Chemistry p. 107 - 121 (2000)
Update date:2022-08-03
Topics:
Younes, Salome
Labssita, Youssef
Baziard-Mouysset, Genevieve
Payard, Marc
Rettori, Marie-Claire
Renard, Pierre
Pfeiffer, Bruno
Caignard, Daniel-Henri
Continuing our previous work that established that some chromones substitued by an aryl alkyl piperazino alkyl side chain are potent and selective sigma ligands and could be interesting in the treatment of psychosis, we synthesized 60 new compounds, replacing the chromone moiety by various cyclic systems. Many derivatives bind to the sigma sites in the nanomolar range and are generally selective in comparison with 5HT(1A) and the D2 receptors. One of the most potent ligands of these series, 1-(2- naphthyl methyl)-4-benzyl piperazine 29, has been studied in various pharmacological tests. Although it doesn't have potential in the treatment of psychosis, the results we obtained confirm the data which indicates that such derivatives could be interesting in the treatment of inflammatory diseases. (C) 2000 Editions scientifiques et medicales Elsevier SAS.
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