Synthesis and evaluation of andrographolide derivatives as potent anti-osteoporosis agents in vitro and in vivo was written by Zhang, Songxuan;Zhang, Yuting;Fang, Yuying;Chen, Hao;Hao, Mengjiao;Tan, Qingyun;Hu, Chen;Zhou, Huihao;Xu, Jun;Gu, Qiong. And the article was included in European Journal of Medicinal Chemistry in 2021.Formula: C4H6N2S This article mentions the following:
In this work, we found that 14-deoxy-11,12-didehydroandrographolide, a derivative of andrographolide, had greatly reduced cytotoxicity compared with andrographolide and exhibited moderate anti-osteoclastogenesis activity. Thirty compounds were synthesized by introducing anti-osteoporosis chemotypes at C-19 of 14-deoxy-11,12-didehydroandrographolide. Six of them exhibited stronger inhibition of osteoclastogenesis than andrographolide. Of note, compound I displayed the most potent activity with IC50 value of 0.35μM. The expression levels of osteoclast-specific genes such as TRAcP, CTSK, NFATc1, and MMP-9 were also decreased by I treatment. Furthermore, Western blot and immunofluorescence analyses demonstrated that I inhibited osteoclast differentiation through downregulation of RANKL-induced NF-κB signaling pathway. In an ovariectomized (OVX) female mice model, I significantly ameliorated bone loss. Therefore, I exhibited promising in vivo efficacy and low toxicity, indicating its therapeutic potential for the treatment of osteoporosis. In the experiment, the researchers used many compounds, for example, Thiazol-2-ylmethanamine (cas: 55661-33-1Formula: C4H6N2S).
Thiazol-2-ylmethanamine (cas: 55661-33-1) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. Thiazole sulfonation occurs only under forcing conditions: the action of oleum at 250 °C for 3 hours in the presence of mercury(II) sulfate leads to 65% formation of 5-thiazole sulfonic acid.Formula: C4H6N2S
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica