Discovery of a highly orally bioavailable c-5-[6-(4-Methanesulfonyloxyphenyl)hexyl]-2-methyl-1,3-dioxane-r-2-carboxylic acid as a potent hypoglycemic and hypolipidemic agent

A series of novel 1,3-dioxane-2-carboxylic acid derivatives containing alkyl chain tether and substituted phenyl group as a lipophilic tail have been prepared as agonists of PPARα and γ. c-5-[6-(4-Methanesulfonyloxyphenyl)hexyl]-2-methyl-1,3-dioxane-r-2-carboxylic acid 13c exhibited potent hypoglycemic and lipid lowering activity with high oral bioavailability in animal models.

Graphical abstractA series of novel 1,3-dioxane-2-carboxylic acid derivatives have been reported as PPARα and γ agonists. Compound 13c exhibited potent hypoglycemic and lipid lowering activity and high oral bioavailability.Figure optionsDownload full-size imageDownload as PowerPoint slide