化学
苯甲酰胺
磺酰
磺胺
三氟甲基
哌嗪
破骨细胞
兰克尔
立体化学
取代基
亲脂性
酰胺
体外
生物化学
有机化学
激活剂(遗传学)
受体
烷基
作者
Alessandra Marie Encarnacion,Nithin Pootheri,Hequan Yao,Zhihao Chen,Sunwoo Lee,Eunae Kim,Tae‐Hoon Lee
标识
DOI:10.1016/j.bmcl.2024.129884
摘要
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 5b emerged as the most effective dose-dependent inhibitor after TRAP staining with an IC
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