A group of 2-methyl-4-phenylquinoline-chalcone analogs (2a-2x) was synthesized and investigated for anti-depressant, anti-inflammatory, and analgesic effects as cyclooxygenase-2 inhibitors. Pharmacological experiments identified 24 analogs that exhibited anti-depressant, anti-inflammatory, and analgesic activities. In particular, compounds 2c, 2k, and 2w markedly shortened immobility times and exhibited the most anti-depressant activity. In addition, the mechanisms of action of the analogs 2c, 2k, and 2w were likely related to increased serotonin levels in the central nervous system. Compounds 2c, 2k, and 2w displayed reasonable cyclooxygenase-2 inhibitory effects (IC50 values from 0.21 to 0.29 µmol/L) similar to celecoxib (IC50: 0.19 µmol/L) in vitro. A molecular docking study of compound 2k also was conducted.

中文翻译：

---

具有抗抑郁，消炎，镇痛和抑制COX-2作用的查尔酮类似物的筛选。

合成了一组2-甲基-4-苯基喹啉-查耳酮类似物（2a-2x），并研究了其作为环加氧酶-2抑制剂的抗抑郁，抗炎和镇痛作用。药理实验确定了24种具有抗抑郁，抗炎和镇痛作用的类似物。特别是，化合物2c，2k和2w显着缩短了固定时间，并表现出最大的抗抑郁活性。此外，类似物2c，2k和2w的作用机制可能与中枢神经系统中5-羟色胺水平的升高有关。化合物2c，2k和2w在体外具有类似于celecoxib（IC50：0.19 µmol / L）的合理的环氧合酶2抑制作用（IC50值为0.21至0.29 µmol / L）。还进行了化合物2k的分子对接研究。