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

Bioorganic & Medicinal Chemistry
2014.0

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.

Knowledge Graph

Similar Paper

Synthesis and pharmacological characterization of 1-benzyl-4-aminoindole-based thyroid hormone receptor β agonists
Bioorganic & Medicinal Chemistry 2014.0
Discovery of novel indane derivatives as liver-selective thyroid hormone receptor β (TRβ) agonists for the treatment of dyslipidemia
Bioorganic & Medicinal Chemistry 2012.0
Design, synthesis, and structure–activity relationship (SAR) of N-[7-(4-hydroxyphenoxy)-6-methylindan-4-yl]malonamic acids as thyroid hormone receptor β (TRβ) selective agonists
Bioorganic & Medicinal Chemistry 2013.0
Synthesis and SAR of potent LXR agonists containing an indole pharmacophore
Bioorganic & Medicinal Chemistry Letters 2009.0
Design, synthesis and biological evaluation of novel TRβ selective agonists sustained by ADME-toxicity analysis
European Journal of Medicinal Chemistry 2020.0
Selective thyroid hormone receptor β agonists with oxadiazolone acid isosteres
Bioorganic & Medicinal Chemistry Letters 2020.0
2-Aryl-N-acyl indole derivatives as liver X receptor (LXR) agonists
Bioorganic & Medicinal Chemistry Letters 2007.0
Discovery of Novel Indazole Derivatives as Highly Potent and Selective Human β<sub>3</sub>-Adrenergic Receptor Agonists with the Possibility of Having No Cardiovascular Side Effects
Journal of Medicinal Chemistry 2015.0
Targeting thyroid hormone receptor-β agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index
Proceedings of the National Academy of Sciences 2007.0
Novel Indole-Based Peroxisome Proliferator-Activated Receptor Agonists:  Design, SAR, Structural Biology, and Biological Activities
Journal of Medicinal Chemistry 2005.0