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 published the artcile< Discovery of N-(4-aryl-5-aryloxy-thiazol-2-yl)-amides as potent RORγt inverse agonists>, Application In Synthesis of 35852-58-5, the main research area is arylaryloxy thiazolyl amide preparation RORt inverse agonist immunomodulator; Crystal structure; RORγt inverse agonists; Th17 cell differentiation; Thiazole ether amides.
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.
Bioorganic & Medicinal Chemistry published new progress about Cell differentiation inducers. 35852-58-5 belongs to class chlorides-buliding-blocks, and the molecular formula is C7H4ClF3O, Application In Synthesis of 35852-58-5.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics