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Novel piperazine-2,5-dione analogs bearing 1H-indole: Synthesis and biological effects
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2020-11-02 , DOI: 10.1016/j.bmcl.2020.127654
Zhehao Huang 1 , Liquan Yin 2 , Liping Guan 3 , Zhaohui Li 1 , Cheng Tan 4
Affiliation  

In this work, a series of novel piperazine-2,5-dione derivatives bearing indole analogs (2a-2q) was designed and synthesized. The synthesized compounds were characterized by IR, 1H NMR, 13C NMR spectroscopy, and ESI-MS. They were then evaluated for their anti-depressant, anti-inflammatory, and analgesic activities in vivo. The experimental results revealed that all the compounds showed clear anti-depressant, anti-inflammatory, and analgesic effects at a dose of 10 mg/kg. Among them, compounds 2e and 2q exhibited the best anti-depressant effects (the percent decreases in the duration of immobility were 70.2% and 71.2%, respectively), which were similar to that of fluoxetine (67.9%) in the forced swim test. Additionally, compounds 2e and 2q also displayed good anti-inflammatory and analgesic activities. Literature reports have highlighted the anti-inflammatory and analgesic effects of anti-depressant drugs, suggesting that they may have a similar mechanism of action. Therefore, further studies to investigate the possible mechanisms of action of compounds 2e and 2q are warranted.



中文翻译:

带有1 H-吲哚的新型哌嗪-2,5-二酮类似物:合成和生物学效应

在这项工作中,设计并合成了一系列带有吲哚类似物(2a-2q)的新型哌嗪-2,5-二酮衍生物。通过IR,1 H NMR,13 C NMR光谱和ESI-MS对合成的化合物进行表征。然后评估它们的体内抗抑郁,抗炎和镇痛活性。实验结果表明,所有化合物在10 mg / kg的剂量下均显示出明显的抗抑郁,抗炎和镇痛作用。其中,化合物2e2q表现出最好的抗抑郁作用(固定时间减少的百分比分别为70.2%和71.2%),与强迫游泳测试中的氟西汀(67.9%)相似。另外,化合物2e2q还显示出良好的抗炎和止痛活性。文献报告强调了抗抑郁药的抗炎和镇痛作用,表明它们可能具有相似的作用机理。因此,有必要进一步研究化合物2e2q的可能作用机理。

更新日期:2020-11-06
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