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含吡唑和嘧啶片段萘醌衍生物的抗惊厥和抗抑郁活性的合成与评价。

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

出版信息

Acta Chim Slov. 2020 Sep;67(3):934-939.

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.

摘要

新型杂环二氯萘醌衍生物通过 2,3-二氯-1,4-萘醌中氯原子取代到吡唑或嘧啶片段合成。这些化合物的结构通过傅里叶变换红外光谱(FT-IR)、电喷雾质谱(ESI-MS)、1H-NMR、13C-NMR 和元素分析得到确认。合成的化合物在戊四氮(PTZ)惊厥模型中评估其抗惊厥作用,在强迫游泳试验(FST)中评估其抗抑郁活性。所有萘醌衍生物在 100mg/kg 剂量下,在口服后 3 小时和 24 小时的 PTZ 诱导试验中表现出抗惊厥作用。此外,与参考药物阿米替林相比,这些化合物具有延长的抗抑郁特性,显著减少了不动时间的持续时间。

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