Discovery of a novel class of PPARδ partial agonists

Anthranilic acid GW9371 was identified as a novel class of PPARδ partial agonist through high-throughput screening. The design and synthesis of SAR analogues is described. GSK1115 and GSK7227 show potent partial agonism of the PPARδ target genes CPT1a and PDK4 in skeletal muscle cells.

Graphical abstractThe discovery and evaluation of a novel anthranilic acid class of PPARδ partial agonists is described.Figure optionsDownload full-size imageDownload as PowerPoint slide