Phenylpropanoic acid derivatives bearing a benzothiazole ring as PPARδ-selective agonists

To find novel PPARδ-selective agonists, we designed and synthesized phenylpropanoic acid derivatives bearing 6-substituted benzothiazoles. Optimization of this series led to the identification of a potent and selective PPARδ agonist 17. Molecular modeling suggested that compound 17 occupies the Y-shaped pocket of PPARδ appropriately.

Graphical abstractTo find novel PPARδ-selective agonists, we designed and synthesized a series of phenylpropanoic acid derivatives bearing a benzothiazole ring. Optimization of this series led to the identification of a potent and selective PPARδ agonist 17.Figure optionsDownload full-size imageDownload as PowerPoint slide