Synthesis And Evaluation On Anticonvulsant And Antidepressant Activities Of Naphthoquinone Derivatives Containing Pyrazole And Pyrimidine Fragments

ACTA CHIMICA SLOVENICA(2020)

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摘要
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, H-1-NMR, C-13-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.
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关键词
2,3-dichloro-1,4-naphthoquinone, pyrazole and pyrimidine fragments, anticonvulsant activity, antidepressant action
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