A total of twenty-two novel coumarin triazole hybrids (4a-4k and 6a-6k) were synthesized from orcinol in good to excellent yields of 70–94%. The structures of all the synthesized compounds were elucidated by spectroscopic techniques such as ¹H NMR, ¹³C NMR, and HRMS. The anti-inflammatory potential of synthesized compounds was investigated against the proinflammatory cytokine, TNF-α on U937 cell line and compounds 4d, 4j, and 6j were found to exhibit promising anti-inflammatory activity. These three compounds were further screened against TNF-α on LPS-stimulated RAW 264.7 cells, which confirm their anti-inflammatory potential. Furthermore, the above said active compounds were tested for their inhibitory effect on RANKL-induced osteoclastogenesis in RAW 264.7 cells by using tartrate resistant acid phosphatase (TRAP) staining assay at 10 µM. Molecular mechanism studies demonstrated that compound 4d exhibited dose dependent inhibition of RANKL-induced osteoclastogenesis by suppression of the NF-kB pathway. Thus, compound 4d is a promising candidate for further optimization to develop as a potent anti-osteoporotic agent.

从二十二烷醇合成了22种新颖的香豆素三唑杂种（4a - 4k和6a - 6k），良率高达70％至94％。通过诸如¹ H NMR，¹³ C NMR和HRMS的光谱技术阐明了所有合成化合物的结构。研究了合成化合物对U937细胞系中促炎细胞因子TNF-α和化合物4d，4j和6j的抗炎潜力被发现表现出有希望的抗炎活性。在LPS刺激的RAW 264.7细胞上进一步针对TNF-α筛选了这三种化合物，证实了它们的抗炎潜力。此外，通过使用10μM的抗酒石酸酸性磷酸酶（TRAP）染色试验，测试了上述活性化合物对RAW 264.7细胞中RANKL诱导的破骨细胞形成的抑制作用。分子机理研究表明，化合物4d通过抑制NF-kB途径对RANKL诱导的破骨细胞生成具有剂量依赖性抑制作用。因此，化合物4d是有希望的候选物，其可以进一步优化发展成为有效的抗骨质疏松剂。