Article ; Online: Expanding the Library of 1,2,4-Oxadiazole Derivatives: Discovery of New Farnesoid X Receptor (FXR) Antagonists/Pregnane X Receptor (PXR) Agonists.
Molecules (Basel, Switzerland)
2023 Volume 28, Issue 6
Abstract: 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 ... ...
| Abstract | 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 |
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| MeSH term(s) | Pregnane X Receptor ; Receptors, Steroid/metabolism ; Receptors, Cytoplasmic and Nuclear ; Molecular Docking Simulation ; Gene Library | |||||
| Chemical Substances | Pregnane X Receptor ; Receptors, Steroid ; Receptors, Cytoplasmic and Nuclear | |||||
| Language | English | |||||
| Publishing date | 2023-03-21 | |||||
| Publishing country | Switzerland | |||||
| Document type | Journal Article | |||||
| ZDB-ID | 1413402-0 | |||||
| ISSN | 1420-3049 ; 1431-5165 ; 1420-3049 | |||||
| ISSN (online) | 1420-3049 | |||||
| ISSN | 1431-5165 ; 1420-3049 | |||||
| DOI | 10.3390/molecules28062840 | |||||
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| Database | MEDical Literature Analysis and Retrieval System OnLINE |
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