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Expanding the Library of 1,2,4-Oxadiazole Derivatives: Discovery of New Farnesoid X Receptor Agonists
Molecules (Basel, Switzerland), 2023-03, Vol.28 (6)
[Peer Reviewed Journal]
COPYRIGHT 2023 MDPI AG ;ISSN: 1420-3049 ;EISSN: 1420-3049 ;DOI: 10.3390/molecules28062840
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Title:
Expanding the Library of 1,2,4-Oxadiazole Derivatives: Discovery of New Farnesoid X Receptor Agonists
Author:
Finamore, Claudia
;
Festa, Carmen
;
Fiorillo, Bianca
;
Leva, Francesco Saverio Di
;
Roselli, Rosalinda
;
Marchianò, Silvia
;
Biagioli, Michele
;
Spinelli, Lucio
;
Fiorucci, Stefano
;
Limongelli, Vittorio
;
Zampella, Angela
;
De Marino, Simona
Subjects:
Medical research
;
Medicine, Experimental
;
Rifaximin
Is Part Of:
Molecules (Basel, Switzerland), 2023-03, Vol.28 (6)
Description:
Compounds featuring a 1,2,4-oxadiazole core have been recently identified as a new chemotype of farnesoid X receptor (FXR) antagonists. With the aim to expand this class of compounds and to understand the building blocks necessary to maintain the antagonistic activity, we describe herein the synthesis, the pharmacological evaluation, and the in vitro pharmacokinetic properties of a novel series of 1,2,4-oxadiazole derivatives decorated on the nitrogen of the piperidine ring with different N-alkyl and N-aryl side chains. In vitro pharmacological evaluation showed compounds 5 and 11 as the first examples of nonsteroidal dual FXR/Pregnane X receptor (PXR) modulators. In HepG2 cells, these compounds modulated PXR- and FXR-regulated genes, resulting in interesting leads in the treatment of inflammatory disorders. Moreover, molecular docking studies supported the experimental results, disclosing the ligand binding mode and allowing rationalization of the activities of compounds 5 and 11.
Publisher:
MDPI AG
Language:
English
Identifier:
ISSN: 1420-3049
EISSN: 1420-3049
DOI: 10.3390/molecules28062840
Source:
DOAJ Directory of Open Access Journals
PubMed Central (Training)
GFMER Free Medical Journals
Alma/SFX Local Collection
ProQuest Central
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