Department of Neurosurgery, China-Japan Union Hospital of Jilin University, Changchun 130033, China.
Rehabilitation Medicine Department, China-Japan Union Hospital of Jilin University, Changchun 130033, China.
Bioorg Med Chem Lett. 2020 Dec 15;30(24):127654. doi: 10.1016/j.bmcl.2020.127654. Epub 2020 Nov 2.
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, H NMR, C 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.
在这项工作中，设计并合成了一系列含有吲哚类似物的新型哌嗪-2,5-二酮衍生物（2a-2q）。通过 IR、H NMR、C NMR 光谱和 ESI-MS 对合成的化合物进行了表征。然后，在体内评估了它们的抗抑郁、抗炎和镇痛活性。实验结果表明，所有化合物在 10mg/kg 剂量下均表现出明显的抗抑郁、抗炎和镇痛作用。其中，化合物 2e 和 2q 表现出最好的抗抑郁作用（不动时间的百分比减少分别为 70.2%和 71.2%），与强迫游泳试验中的氟西汀（67.9%）相似。此外，化合物 2e 和 2q 还表现出良好的抗炎和镇痛活性。文献报道强调了抗抑郁药物的抗炎和镇痛作用，表明它们可能具有类似的作用机制。因此，有必要进一步研究化合物 2e 和 2q 的可能作用机制。
