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Bioorg Med Chem Lett ; 29(14): 1799-1806, 2019 07 15.
Article in English | MEDLINE | ID: mdl-31101472

ABSTRACT

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 sulphonamides 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 biological activity of these derivatives is described herein.


Subject(s)
Drug Inverse Agonism , Nuclear Receptor Subfamily 1, Group F, Member 3/chemistry , Quinolines/chemistry , Animals , Disease Models, Animal , Humans , Mice
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