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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Veröffentlicht in:	Bioorganic & medicinal chemistry 2014-01, Vol.22 (1), p.488-498
Hauptverfasser:	Takahashi, Naoki, Maeda, Koji, Asano, Yukiyasu, Watanabe, Nobuhide
Format:	Artikel
Sprache:	eng
Schlagworte:	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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Beschreibung
Zusammenfassung:	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