Next Article in Journal
In House Validated UHPLC Protocol for the Determination of the Total Hydroxytyrosol and Tyrosol Content in Virgin Olive Oil Fit for the Purpose of the Health Claim Introduced by the EC Regulation 432/2012 for “Olive Oil Polyphenols”
Next Article in Special Issue
Characterization and Antibacterial Activity of 7S and 11S Globulins Isolated from Cowpea Seed Protein
Previous Article in Journal
Effects of Maltodextrins on the Kinetics of Lycopene and Chlorogenic Acid Degradation in Dried Tomato
Previous Article in Special Issue
Simultaneous Quantification of L-Arginine and Monosaccharides during Fermentation: An Advanced Chromatography Approach
Article Menu

Export Article

Open AccessArticle
Molecules 2019, 24(6), 1043; https://doi.org/10.3390/molecules24061043

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

1
Department of Pharmacy, University of Naples "Federico II", via D. Montesano 49, 80131 Naples, Italy
2
Department of Surgery and Biomedical Sciences, Nuova Facoltà di Medicina, Piazza Lucio Severi, 1 - 06132 Perugia, Italy
3
Department of Pharmacy, University of Salerno, Via Giovanni Paolo II, 132, 84084 Fisciano, Salerno, Italy
4
Università della Svizzera italiana (USI), Faculty of Biomedical Sciences, Institute of Computational Science - Center for Computational Medicine in Cardiology, Via G. Buffi 13, CH-6900 Lugano, Switzerland
*
Author to whom correspondence should be addressed.
Academic Editors: Giorgia Oliviero and Nicola Borbone
Received: 11 February 2019 / Revised: 11 March 2019 / Accepted: 12 March 2019 / Published: 16 March 2019
(This article belongs to the Special Issue Molecules for Biotechnologies)
Full-Text   |   PDF [2008 KB, uploaded 16 March 2019]   |  
  |   Review Reports

Abstract

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. View Full-Text
Keywords: FXR agonists; bile acid receptors; steroidal scaffolds; medicinal chemistry FXR agonists; bile acid receptors; steroidal scaffolds; medicinal chemistry
Figures

Graphical abstract

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

Supplementary material

SciFeed

Share & Cite This Article

MDPI and ACS Style

Finamore, C.; Baronissi, G.; Marchianò, S.; Di Leva, F.S.; Carino, A.; Monti, M.C.; Limongelli, V.; Zampella, A.; Fiorucci, S.; Sepe, V. Introduction of Nonacidic Side Chains on 6-Ethylcholane Scaffolds in the Identification of Potent Bile Acid Receptor Agonists with Improved Pharmacokinetic Properties. Molecules 2019, 24, 1043.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top