1000604-24-9Relevant academic research and scientific papers
Design and synthesis of a novel series of [1-(4-hydroxy-benzyl)-1H-indol-5-yloxy]-acetic acid compounds as potent, selective, thyroid hormone receptor β agonists
Burkholder, Timothy P.,Cunningham, Brian E.,Clayton, Joshua R.,Lander, Peter A.,Brown, Matthew L.,Doti, Robert A.,Durst, Gregory L.,Montrose-Rafizadeh, Chahrzad,King, Constance,Osborne, Harold E.,Amos, Robert M.,Zink, Richard W.,Stramm, Lawrence E.,Burris, Thomas P.,Cardona, Guemalli,Konkol, Debra L.,Reidy, Charles,Christe, Michael E.,Genin, Michael J.
, p. 1377 - 1380 (2015/03/30)
The design, synthesis, and structure activity relationships for a novel series of indoles as potent, selective, thyroid hormone receptor β (TRβ) agonists is described. Compounds with >50× binding selectivity for TRβ over TRα were generated and evaluation of compound 1c from this series in a model of dyslipidemia demonstrated positive effects on plasma lipid endpoints in vivo.
Synthesis and pharmacological characterization of 1-benzyl-4-aminoindole- based thyroid hormone receptor β agonists
Takahashi, Naoki,Maeda, Koji,Asano, Yukiyasu,Watanabe, Nobuhide
, p. 488 - 498 (2014/01/17)
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.
NOVEL 6-5 BICYCIC HETEROCYCLIC DERIVATIVE AND MEDICAL USE THEREOF
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Page/Page column 43, (2009/04/23)
An object of the present invention is to provide a medicament as a thyroid hormone receptor ligand which is sufficient in drug efficacy and safety, and has the excellent action as a drug. The present invention provides a compound represented by the following general formula (I) or a pharmaceutically acceptable salt thereof: [wherein [Chemical Formula 2] is a single bond or a double bond; A is -CH2- or -CO-; X, Y, and Z are each independently a nitrogen atom or a carbon atom; R1 is a hydrogen atom or an aralkyl group; R2 is an alkyl group or an aralkyl group, etc.; R3 is a hydrogen atom or an alkyl group, etc.; R4 is a hydrogen atom or an alkyl group; R5 is a hydrogen atom, an alkyl group or a halo lower alkyl group, etc.; R6 is a hydrogen atom or an alkyl group; R7 is a hydrogen atom, etc.; R8 is a hydrogen atom, or an alkyl group, etc.; and E is -NHCO-G-COR12, etc. (wherein G is a single bond or an alkylene group, and R12 is a hydroxy group or an alkoxy group)].
