Introduction of Nonacidic Side Chains on 6-Ethylcholane Scaffolds in the Identification of Potent Bile Acid Receptor Agonists with Improved Pharmacokinetic Properties

Autor:	Claudia Finamore, Giuliana Baronissi, Silvia Marchianò, Francesco Saverio Di Leva, Adriana Carino, Maria Chiara Monti, Vittorio Limongelli, Angela Zampella, Stefano Fiorucci, Valentina Sepe
Jazyk:	angličtina
Rok vydání:	2019
Předmět:	FXR agonists bile acid receptors steroidal scaffolds medicinal chemistry Organic chemistry QD241-441
Zdroj:	Molecules, Vol 24, Iss 6, p 1043 (2019)
Druh dokumentu:	article
ISSN:	1420-3049
DOI:	10.3390/molecules24061043
Popis:	As a cellular bile acid sensor, farnesoid X receptor (FXR) and the membrane G-coupled receptor (GPBAR1) participate in maintaining bile acid, lipid, and glucose homeostasis. To date, several selective and dual agonists have been developed as promising pharmacological approach to metabolic disorders, with most of them possessing an acidic conjugable function that might compromise their pharmacokinetic distribution. Here, guided by docking calculations, nonacidic 6-ethyl cholane derivatives have been prepared. In vitro pharmacological characterization resulted in the identification of bile acid receptor modulators with improved pharmacokinetic properties.
Databáze:	Directory of Open Access Journals
Externí odkaz:	https://doaj.org/article/902c71cfe74b4ac3abdea972db5a5b09 Zobrazit plný text záznamu View record in DOAJ Plný text ve formátu PDF Plný text ve formátu HTML
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