On February 1, 2020, Sun, Nannan; Ma, Xiaojun; Zhou, Kaifeng; Zhu, Chen; Cao, Zhonglian; Wang, Yonghui; Xu, Jun; Fu, Wei published an article.Reference of 4-(Bromomethyl)-1,1′-biphenyl The title of the article was Discovery of novel N-sulfonamide-tetrahydroquinolines as potent retinoic acid receptor-related orphan receptor γt inverse agonists for the treatment of autoimmune diseases. And the article contained the following:
In this study, authors designed and synthesized a series of N-sulfonamide-tetrahydroquinolines by mol. modeling and scaffold hopping strategy, aiming at improving the metabolic stabilities. Detailed SAR exploration led to identification of potent RORγt inverse agonists such as compound II with moderate binding affinity and inhibitory activity of Th17 cell differentiation. Binding mode of compound II with RORγt-LBD was revealed by mol. docking. Moreover, compound II showed lower intrinsic clearance in mouse liver microsomes compared with compound I and potent in-vivo efficacy and safety in psoriasis models, which can be used as a good starting point for the further optimization. The experimental process involved the reaction of 4-(Bromomethyl)-1,1′-biphenyl(cas: 2567-29-5).Reference of 4-(Bromomethyl)-1,1′-biphenyl
The Article related to sulfonamido tetrahydroquinoline preparation rror inverse agonist sar safety, inverse agonists, metabolic stability, n-sulfonamide-tetrahydroquinolines, psoriasis, retinoic acid receptor-related orphan receptor γt (rorγt), th17 cells and other aspects.Reference of 4-(Bromomethyl)-1,1′-biphenyl
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary