Amaudrut, Jerome; Argiriadi, Maria A.; Barth, Martine; Breinlinger, Eric C.; Bressac, Didier; Broqua, Pierre; Calderwood, David J.; Chatar, Mohamed; Cusack, Kevin P.; Gauld, Stephen B.; Jacquet, Sebastien; Kamath, Rajesh V.; Kort, Michael E.; Lepais, Valerie; Luccarini, Jean-Michel; Masson, Philippe; Montalbetti, Christian; Mounier, Laurent; Potin, Dominique; Poupardin, Olivia; Rouaud, Sylvie; Spitzer, Luc; Wallace, Craig D. published the artcile< Discovery of novel quinoline sulphonamide derivatives as potent, selective and orally active RORγ inverse agonists>, Category: imidazoles-derivatives, the main research area is RORgamma agonist IL17 nuclear hormone receptor SAR; IL-17; Nuclear hormone receptor; RORγt inverse agonist; SAR; Th17 cells.
A high-throughput screen against Inventiva’s compound library using a Gal4/RORγ-LBD luciferase reporter gene assay led to the discovery of a new series of quinoline sulfonamides as RORγ inhibitors, eventually giving rise to a lead compound having an interesting in vivo profile after oral administration. This lead was evaluated in a target engagement model in mouse, where it reduced IL-17 cytokine production after immune challenge. It also proved to be active in a multiple sclerosis model (EAE) where it reduced the disease score. The synthesis, structure activity relationship (SAR) and biol. activity of these derivatives is described herein.
Bioorganic & Medicinal Chemistry Letters published new progress about Autoimmune disease. 1003-21-0 belongs to class imidazoles-derivatives, and the molecular formula is C4H5BrN2, Category: imidazoles-derivatives.
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem