Both cyclopropyl amide and piperazine sulfonamide functional groups are known for their various biological properties used for drug development. Herein, we synthesized nine new derivatives with different substituent groups incorporating these moieties and screened them for their anti-osteoclast differentiation activity. After analyzing the structure–activity relationship (SAR), the inhibitory effect against osteoclastogenesis was determined to be dependent on the lipophilicity of the compound. Derivative emerged as the most effective dose-dependent inhibitor after TRAP staining with an IC of 0.64 µM against RANKL-induced osteoclast cells. was also able to suppress F-acting ring formation and bone resorption activity of osteoclasts in vitro. Finally, well-acknowledged gene and protein osteoclast-specific marker expression levels were decreased after administration on primary murine osteoclast cells.

中文翻译：

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新型抑制剂 N-环丙基-4-((4-((4-(三氟甲基)苯基)磺酰基)哌嗪-1-基)甲基)苯甲酰胺在体外减弱 RANKL 介导的破骨细胞分化


环丙基酰胺和哌嗪磺酰胺官能团都因其用于药物开发的各种生物学特性而闻名。在此，我们合成了九种具有不同取代基并结合这些部分的新衍生物，并筛选了它们的抗破骨细胞分化活性。分析构效关系（SAR）后，确定对破骨细胞生成的抑制作用取决于化合物的亲脂性。 TRAP 染色后，衍生物成为最有效的剂量依赖性抑制剂，对 RANKL 诱导的破骨细胞的 IC 值为 0.64 µM。还能够在体外抑制破骨细胞的 F 作用环形成和骨吸收活性。最后，在原代小鼠破骨细胞上给药后，众所周知的基因和蛋白质破骨细胞特异性标志物表达水平降低。