Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 26, Issue 2, Pages 483-500Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2017.12.006
Keywords
Retinoic acid receptor-related orphan receptor-gamma t (ROR gamma t); Inverse agonist; Autoimmune disease; Th17; IL-17; Phenylglycinamide
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A series of novel phenylglycinamides as retinoic acid receptor-related orphan receptor-gamma t (ROR gamma t) inverse agonists were discovered through optimization of a high-throughput screen hit 1. (R)-N-(2-((3,5-Difluoro-4-(trimethylsilyl)phenyl) amino)-1-(4-methoxyphenyl)-2-oxoethyl)-3-hydroxy-N-methylisoxazole-5-carboxamide (22) was identified as one of the best of these compounds. It displayed higher subtype selectivity and specificity over other nuclear receptors and demonstrated in vivo potency to suppress the transcriptional activity of ROR gamma t in a mouse PD (pharmacodynamic) model upon oral administration. (C) 2017 Elsevier Ltd. All rights reserved.
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