Title of article
N-Benzyl-N-(pyrrolidin-3-yl)carboxamides as a new class of selective dual serotonin/noradrenaline reuptake inhibitors
Author/Authors
Florian Wakenhut، نويسنده , , Paul V. Fish، نويسنده , , M. Jonathan Fray، نويسنده , , Ian Gurrell، نويسنده , , James E. Mills، نويسنده , , Alan Stobie، نويسنده , , Gavin A. Whitlock، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
4
From page
4308
To page
4311
Abstract
The structure–activity relationship and the synthesis of novel N-benzyl-N-(pyrrolidin-3-yl)carboxamides as dual serotonin (5-HT) and noradrenaline (NA) monoamine reuptake inhibitors are described. Compounds such as 18 exhibited dual 5-HT and NA reuptake inhibition, good selectivity over dopamine (DA) reuptake inhibition and drug-like physicochemical properties consistent with CNS target space. Compound 18 was selected for further preclinical evaluation.
Keywords
Serotonin reuptake , N-benzyl-N-(pyrrolidin-3-yl)carboxamides , Noradrenaline reuptake , metabolic profile , Metabolic stability , CYP2D6 inhibition , Lipophilicity , SNRI
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799770
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