2. Academic Validation
  3. Synthesis and pharmacological characterization of 1-benzyl-4-aminoindole-based thyroid hormone receptor β agonists

Synthesis and pharmacological characterization of 1-benzyl-4-aminoindole-based thyroid hormone receptor β agonists

  • Bioorg Med Chem. 2014 Jan 1;22(1):488-98. doi: 10.1016/j.bmc.2013.11.001.
Naoki Takahashi 1,  Koji Maeda 1,  Yukiyasu Asano 2,  Nobuhide Watanabe 3
Affiliations

Affiliations

  • 1 Drug Discovery Laboratories, Sanwa Kagaku Kenkyusho Co., Ltd, 363 Shiosaki, Hokusei-cho, Inabe-city, Mie 511-0406, Japan.
  • 2 Product Planning II, R&D Planning Department, R&D Strategy Center, Sanwa Kagaku Kenkyusho Co., Ltd, 35 Higashisotobori-cho, Higashi-ku, Nagoya 461-8631, Japan.
  • 3 Drug Discovery Laboratories, Sanwa Kagaku Kenkyusho Co., Ltd, 363 Shiosaki, Hokusei-cho, Inabe-city, Mie 511-0406, Japan. Electronic address: no_watanabe@skk-net.com.
PMID: 24290064 DOI: 10.1016/j.bmc.2013.11.001
Abstract

A series of 1-benzylindole-based TRβ agonists were prepared and evaluated. Compounds 11b' and 11c' were found to have cholesterol-lowering in a rat model with marginal effects on cardiac function and HPT axis. The present work illustrates the potential use of indoles as inner ring isosteres.

Keywords

Dyslipidemia; Hypothalamic/pituitary/thyroid axis; Thyroid hormone receptor β agonists; Thyroid stimulating hormone.

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