We report the synthesis and evaluation of a novel PPARδ agonist, compound 12a, characterized by a benzisoxazole ring. Compound 12a exhibited a potent human PPARδ transactivation activity (EC50: 0.011 μM). Preliminary biological testing suggests that compound 12a has significant HDL-cholesterol elevating effect in an animal model of dyslipidemia.
Keywords: HDL Cholesterol, PPARδ Agonist, Compound 12a, Benzisoxazole ring, Transactivation, Obesity, Diabetes, Lipoprotein, Proliferator-Activated, Receptor, Peroxisome, atherosclerotic cardiovascular disease, dyslipidemia, niacin, apolipoprotein A-I Milano/phospholipid complex, Ames test
Rights & PermissionsPrintExport