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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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

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

Volume 8, Issue 6, 2011

Page: [496 - 499] Pages: 4

DOI: 10.2174/157018011795906802

Price: $65


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

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