The currently used treatment of central nervous system diseases, including depression, schizophrenia or Parkinson's disease, is ineffective. Commonly available drugs exhibit a vast number of adverse effects; and even as much as 30% of patients do not respond to the therapy. Therefore, there still exists a need for researching antidepressants even further. [1,2] Having analysed prior art literature, we selected a group of poorly investigated compounds, namely aminotriazines. Aminotriazines have been described as compounds acting only on 5-HT7 receptor. [3] However, the involvement of the 5-HT7 receptor only may lead to successfully diminishing depression symptoms. As a part of our research, we developed the tryptamine moiety with an aminotriazine core. The new compounds were obtained via solvent-free reactions supported by a microwave irradiation. This approach can be considered as a fast, efficient method, consistent with the trends of green chemistry. The final product was purified by crystallization or by chromatography. New compounds were elucidated using molecular modelling (docking and molecular dynamic). The calculated physicochemical parameters determining the properties of drug-like compounds were also considered. Each of the ligands obtained was tested in in vitro assay for binding to the 5-HT7. Additional drug-drug interaction, metabolic patchways and hepatotoxicity have been studied. The preliminary results of biological tests for aminotriazine derivatives show that the compounds exhibit a very good affinity to 5-HT7 receptor only.

Design, synthesis and biological activity of new aminotriazine derivatives as selective 5-HT7 receptor ligands

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.