Novel 1-(2-pyrimidin-2-yl)piperazine derivatives as selective monoamine oxidase (MAO)-A inhibitors

作者：Kaya Betul; Yurttas Leyla^*; Saglik Begum Nurpelin; Levent Serkan; Ozkay Yusuf; Kaplancikli Zafer Asim

来源：Journal of Enzyme Inhibition and Medicinal Chemistry, 2017, 32(1): 193-202.

DOI：10.1080/14756366.2016.1247054

• Depression
• Lipinski's rule of five
• Molinspiration
• MolSoft
• monoamine oxidase A
• (2-pyrimidinyl)piperazine

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.

• 出版日期2017