Discovery of N-(4-aryl-5-aryloxy-thiazol-2-yl)-amides as potent RORγt inverse agonists was written by Wang, Yonghui;Yang, Ting;Liu, Qian;Ma, Yingli;Yang, Liuqing;Zhou, Ling;Xiang, Zhijun;Cheng, Ziqiang;Lu, Sijie;Orband-Miller, Lisa A.;Zhang, Wei;Wu, Qianqian;Zhang, Kathleen;Li, Yi;Xiang, Jia-Ning;Elliott, John D.;Leung, Stewart;Ren, Feng;Lin, Xichen. And the article was included in Bioorganic & Medicinal Chemistry in 2015.Formula: C15H12N2S This article mentions the following:
A novel series of N-(4-aryl-5-aryloxy-thiazol-2-yl)-amides as RORγt inverse agonists was discovered. Binding mode anal. of a RORγt partial agonist (2c) revealed by co-crystal structure in RORγt LBD suggests that the inverse agonists do not directly interfere with the interaction between H12 and the RORγt LBD. Detailed SAR exploration led to identification of potent RORγt inverse agonists such as 3m with a pIC50 of 8.0. Selected compounds in the series showed reasonable activity in Th17 cell differentiation assay as well as low intrinsic clearance in mouse liver microsomes. In the experiment, the researchers used many compounds, for example, 4,5-Diphenylthiazol-2-amine (cas: 6318-74-7Formula: C15H12N2S).
4,5-Diphenylthiazol-2-amine (cas: 6318-74-7) belongs to thiazole derivatives. The thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone. 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: C15H12N2S
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica