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Synthesis and Evaluation on Anticonvulsant and Antidepressant Activities of Naphthoquinone Derivatives Containing Pyrazole and Pyrimidine Fragments

Nataliia Polish, Mariia Nesterkina, Nataliia Marintsova, Andriy Karkhut, Iryna Kravchenko, Volodymyr Novikov, Andrei Khairulin

Abstract


Novel heterocyclic dichloronaphthoquinone derivatives have been synthesized by chlorine atom substitution in 2,3-dichloro-1,4-naphthoquinone to pyrazole or pyrimidine fragments. The structures of these compounds have been confirmed by FT-IR, ESI-MS, 1H‐NMR, 13C-NMR and elementary analysis. Synthesized compounds were evaluated for their anticonvulsant action in a pentylenetetrazole (PTZ)-convulsion model and antidepressant activity in the forced swimming test (FST). All naphthoquinone derivatives at a dose 100 mg/kg indicated anticonvulsant effect in PTZ-induced test at 3 h and 24 h after oral administration. In addition, these compounds possessed prolonged antidepressant properties significantly reducing the duration of immobility time when compared to the reference drug amitriptyline.  


Keywords


2,3-dichloro-1,4-naphthoquinone; pyrazole and pyrimidine fragments; anticonvulsant activity; antidepressant action

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DOI: http://dx.doi.org/10.17344/acsi.2020.5938

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Copyright (c) 2020 Mariia Nesterkina, Nataliia Polish, Nataliia Marintsova, Andriy Karkhut, Iryna Kravchenko, Volodymyr Novikov, Andrei Khairulin

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