Discovery of novel indane derivatives as liver-selective thyroid hormone receptor β (TRβ) agonists for the treatment of dyslipidemia

H Shiohara, T Nakamura, N Kikuchi, T Ozawa…

Index: Shiohara, Hiroaki; Nakamura, Tetsuya; Kikuchi, Norihiko; Ozawa, Tomonaga; Nagano, Ryuichi; Matsuzawa, Akane; Ohnota, Hideki; Miyamoto, Takahide; Ichikawa, Kazuo; Hashizume, Kiyoshi Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 11 p. 3622 - 3634

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Citation Number: 19

Abstract

Thyromimetics that specifically target TRβ have been shown to reduce plasma cholesterol levels and avoid atherosclerosis through the promotion of reverse cholesterol transport in an animal model. We designed novel thyromimetics with high receptor (TRβ) and organ (liver) selectivity based on the structure of eprotirome (3) and molecular modeling. We found that indane derivatives are potent and dual-selective thyromimetics expected to avoid ...