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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: Geneva Foundation Free Medical Journals at publisher websites
    PubMed Central
    Directory of Open Access Journals
    Alma/SFX Local Collection
    ProQuest Central
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