Discovery and structural optimization of 4-(4-(benzyloxy)phenyl)-34-dihydropyrimidin-2(1H)-ones as RORc inverse agonists

摘要

Aim:Retinoic acid receptor-related orphan nuclear receptors (RORs) are orphan nuclear receptors that show constitutive activity in the absence of ligands. Among 3 subtypes of RORs, RORc is a promising therapeutic target for the treatment of Th17-mediated autoimmune diseases. Here, we report novel RORc inverse agonists discovered through structure-based drug design.