Discovery and pharmacological evaluation of indole derivatives as potent and selective RORγt inverse agonist for multiple autoimmune conditions.
Bioorganic & Medicinal Chemistry Letters(2019)
摘要
•Identification of indole analogues as potent RORγt inverse agonists, SAR of around 44 compounds is presented.•Potent compounds were evaluated for pharmacokinetic properties and data is presented.•Significant inhibition of anti-CD3/anti-CD28 induced Il17 gene expression in mouse splenocytes assay.•One of the potent compounds, RO-2 inhibited IL-17A release from (a) mouse splenocytes and (b) human whole blood with an IC50 of 503 nM and 490 nM respectively.•RO-2 was evaluated for its potential in experimental autoimmune encephalomyelitis (EAE) and psoriasis model.
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IUHZJIRXCFINGV-UHFFFAOYSA-N
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