Design of novel multiple-acting ligands towards SERT and 5-HT sub(2C) receptors

Design of novel multiple-acting ligands towards SERT and 5-HT sub(2C) receptors

This Letter describes our attempts to elaborate dually acting compounds possessing serotonin re-uptake transporter inhibitor and serotonin 5-HT sub(2C) receptor antagonist properties. A novel series of 1,3-diphenylureas and N-phenylbenzamides have thus been prepared and evaluated. Based on its in vi...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters Vol. 24; no. 9; pp. 2118 - 2122
Main Authors: Elias, Oliver, Agai-Csongor, Eva, Domany, Gyorgy, Keserue, Gyorgy Miklos, Gere, Aniko, Kiss, Bela, Hellinger, Eva, Vastag, Monika, Gyertyan, Istvan
Format: Journal Article
Language:English
Published: 01-05-2014
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Summary:This Letter describes our attempts to elaborate dually acting compounds possessing serotonin re-uptake transporter inhibitor and serotonin 5-HT sub(2C) receptor antagonist properties. A novel series of 1,3-diphenylureas and N-phenylbenzamides have thus been prepared and evaluated. Based on its in vitro and in vivo activities, as well as pharmacokinetic profile, compound 16a was identified as a lead compound. The synthesis and structure-activity relationship of this series of compounds is presented herein.
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ISSN:0960-894X
DOI:10.1016/j.bmcl.2014.03.043