Journal
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
Volume 32, Issue 1, Pages 193-202Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756366.2016.1247054
Keywords
Depression; Lipinski's rule of five; Molinspiration; MolSoft; monoamine oxidase A; (2-pyrimidinyl)piperazine
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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 mu M, 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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