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

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.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2014-01, Vol.22 (1), p.488-498
Main Authors: Takahashi, Naoki, Maeda, Koji, Asano, Yukiyasu, Watanabe, Nobuhide
Format: Article
Language:English
Subjects:
Animals
Dyslipidemia
Hypothalamic/pituitary/thyroid axis
Indoles - chemical synthesis
Indoles - pharmacology
Rats
Thyroid hormone receptor β agonists
Thyroid Hormone Receptors beta - agonists
Thyroid Hormone Receptors beta - drug effects
Thyroid stimulating hormone
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Description
Summary: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.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2013.11.001