Design and synthesis of oxime ethers of α-acyl-β-phenylpropanoic acids as PPAR dual agonists

Oxime ethers of α-acyl-β-phenylpropanoic acids were prepared to apply as PPARα and γ dual agonists. Among them, compound 11l proved to exhibit potent in vitro activities with EC50 of 19 and 13 nM in PPARα and γ, respectively. It showed better glucose lowering effects than rosiglitazone 1 and ameliorated the lipid profile like plasma triglyceride in db/db mice model.

Graphical abstractCompound 11l exhibited potent in vitro activities in PPARα and γ (EC50 = 19, 13 nM). It showed better glucose lowering effect than rosiglitazone as well.Figure optionsDownload full-size imageDownload as PowerPoint slide