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

Autor:	Stramm Lawrence E, Constance King, Debra L. Konkol, Thomas P. Burris, Chahrzad Montrose-Rafizadeh, Burkholder Timothy P, Harold E. Osborne, Brian Eugene Cunningham, Charles Reidy, Peter Ambrose Lander, Joshua Ryan Clayton, Robert M. Amos, Guemalli R. Cardona, Matthew L. Brown, Michael E. Christe, Michael James Genin, Robert Anthony Doti, Richard W. Zink, Gregory L. Durst
Rok vydání:	2014
Předmět:	Agonist Models Molecular Indoles medicine.drug_class Clinical Biochemistry Pharmaceutical Science Acetates Biochemistry Thyroid hormone receptor beta Acetic acid chemistry.chemical_compound Structure-Activity Relationship In vivo Drug Discovery Plasma lipids medicine Humans Molecular Biology Binding selectivity Indole test Thyroid hormone receptor Dose-Response Relationship Drug Molecular Structure Organic Chemistry Thyroid Hormone Receptors beta chemistry Drug Design Molecular Medicine
Zdroj:	Bioorganicmedicinal chemistry letters. 25(7)
ISSN:	1464-3405
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::951a2935a45ecc576b4b6f4da15095f9 https://pubmed.ncbi.nlm.nih.gov/25752984 Zobrazit plný text záznamu Full Text from ScienceDirect