226942-29-6, In an article, published in an article,authors is Cao, Zhonglian, once mentioned the application of 226942-29-6, Name is 6-Bromo-1,2,3,4-tetrahydroisoquinoline,molecular formula is C9H10BrN, is a conventional compound. this article was the specific content is as follows.
Discovery of novel N-sulfonamide-tetrahydroquinolines as potent retinoic acid receptor-related orphan receptor gammat inverse agonists for the treatment of autoimmune diseases
Targeting the nuclear receptor RORgammat is thought to be effective in autoimmune disorders. Tertiary sulfonamide 1 was found to be a potent RORgammat inverse agonist previously. However, the high hepatic clearance value limits its druggability. In this study, we designed and synthesized a series of N-sulfonamide-tetrahydroquinolines by molecular modeling and scaffold hopping strategy, aiming at improving the metabolic stabilities. Detailed SAR exploration led to identification of potent RORgammat inverse agonists such as 13 with moderate binding affinity and inhibitory activity of Th17 cell differentiation. Binding mode of 13 with RORgammat-LBD was revealed by molecular docking. Moreover, 13 showed lower intrinsic clearance in mouse liver microsomes compared with 1 and potent in vivo efficacy and safety in psoriasis models, which can be used as a good starting point for the further optimization.
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Reference£º
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem