High-Density Lipoprotein Cholesterol-Elevating Effect of a Novel Peroxisome Proliferator-Activated Receptor δ Agonist

Title: High-Density Lipoprotein Cholesterol-Elevating Effect of a Novel Peroxisome Proliferator-Activated Receptor δ Agonist

Volume: 8 Issue: 6

Author(s): Shogo Sakuma, Tsuyoshi Endo, Takashi Kanda, Hideki Nakamura, Satomi Yamasaki and Tomio Yamakawa

Affiliation:

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

Abstract: 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.

Cite this article as:

Sakuma Shogo, Endo Tsuyoshi, Kanda Takashi, Nakamura Hideki, Yamasaki Satomi and Yamakawa Tomio, High-Density Lipoprotein Cholesterol-Elevating Effect of a Novel Peroxisome Proliferator-Activated Receptor δ Agonist, Letters in Drug Design & Discovery 2011; 8 (6) . https://dx.doi.org/10.2174/157018011795906802