Novel 1-(2-pyrimidin-2-yl)piperazine derivatives as selective monoamine oxidase (MAO)-A inhibitors |
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Authors: | Betül Kaya Begüm Nurpelin Sağlik Serkan Levent Yusuf Özkay Zafer Asim Kaplancikli |
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Affiliation: | 1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, Eski?ehir, Turkey;2. Doping and Narcotic Compounds Analysis Laboratory, Faculty of Pharmacy, Anadolu University, Eski?ehir, Turkey |
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Abstract: | In the present study, a new series of 2-[4-(pyrimidin-2-yl)piperazin-1-yl]-2-oxoethyl 4-substituted piperazine-1-carbodithioate derivatives (2a-n) were synthesized and screened for their monoamine oxidase A and B inhibitory activity. The structures of compounds were elucidated using spectroscopic methods and some physicochemical properties of new compounds were predicted using Molinspiration and MolSoft programs. Compounds 2-[4-(pyrimidin-2-yl)piperazin-1-yl]-2-oxoethyl 4-(4-nitrophenyl)piperazine-1-carbodithioate (2j) and 2-[4-(pyrimidin-2-yl)piperazin-1-yl]-2-oxoethyl 4-benzhydrylpiperazine-1-carbodithioate (2m) exhibited selective MAO-A inhibitory activity with IC50?=?23.10, 24.14?µM, respectively. Some of the biological results were found in accordance with the obtained in silico data based on Lipinski’s fule of five. |
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Keywords: | Depression Lipinski’s rule of five Molinspiration MolSoft monoamine oxidase A (2-pyrimidinyl)piperazine |
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