Conformationally constrained farnesoid X receptor (FXR) agonists: alternative replacements of the stilbene

Autor:	Aaron B. Miller, Harry B. Marr, Katrina L. Creech, G. Bruce Wisely, Shawn P. Williams, Adwoa Akwabi-Ameyaw, Lihong Chen, David N. Deaton, Justin A. Caravella, Paul Kenneth Spearing, Kevin P. Madauss, Derek J. Parks, Frank Navas, Dan Todd
Rok vydání:	2011
Předmět:	Agonist Stereochemistry medicine.drug_class Clinical Biochemistry Molecular Sequence Data Molecular Conformation Pharmaceutical Science Receptors Cytoplasmic and Nuclear Biochemistry Cell Line chemistry.chemical_compound Drug Discovery Stilbenes medicine Moiety Animals Humans Carboxylate Amino Acid Sequence Molecular Biology Indole test Organic Chemistry Benzothiophene Isoxazoles G protein-coupled bile acid receptor chemistry Molecular Medicine Farnesoid X receptor Transcription regulator
Zdroj:	Bioorganicmedicinal chemistry letters. 21(20)
ISSN:	1464-3405
Popis:	To further explore the optimum placement of the acid moiety in conformationally constrained analogs of GW 4064 1a, a series of stilbene replacements were prepared. The benzothiophene 1f and the indole 1g display the optimal orientation of the carboxylate for enhanced FXR agonist potency.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7f939259f5c374490a071b94fee47ab3 https://pubmed.ncbi.nlm.nih.gov/21890356 Zobrazit plný text záznamu Full Text from ScienceDirect