ArticleScientific reports2019
Discovery of ((1,2,4-oxadiazol-5-yl)pyrrolidin-3-yl)ureidyl derivatives as selective non-steroidal agonists of the G-protein coupled bile acid receptor-1.
Article in Scientific reports, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 16 citations in OpenAlex.
- From Structure to Dynamics: Activation Mechanism of the G Protein-Coupled Bile Acid Receptor 1‑GACS omega · 2026Article
- The Role of Five-Membered Aromatic Rings Containing N and O in Modulating Bile Acid Receptors: An Overview.ChemMedChem · 2025Review
- The discovery of a new nonbile acid modulator of Takeda G protein-coupled receptor 5: An integrated computational approach.Archiv der Pharmazie · 2025Article
- Room Temperature Synthesis of Bioactive 1,2,4-Oxadiazoles.International journal of molecular sciences · 2023Review
- Bile Acids: Physiological Activity and Perspectives of Using in Clinical and Laboratory Diagnostics.Molecules (Basel, Switzerland) · 2022Review
- Discovery of a Potent and Orally Active Dual GPBAR1/CysLTFrontiers in pharmacology · 2022Article
- Article
- Synergism of a Novel 1,2,4-oxadiazole-containing Derivative with Oxacillin against Methicillin-ResistantAntibiotics (Basel, Switzerland) · 2021Article
- The Liver under the Spotlight: Bile Acids and Oxysterols as Pivotal Actors Controlling Metabolism.Cells · 2021Review
- DDT - Drug Discovery Tool: a fast and intuitive graphics user interface for docking and molecular dynamics analysis.Bioinformatics (Oxford, England) · 2019Article
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Authors and funding
11 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The G-protein bile acid receptor 1 (GPBAR1) has emerged in the last decade as prominent target for the treatment of metabolic and inflammatory diseases including type 2 diabetes, obesity, and non-alcoholic steatohepatitis. To date numerous bile acid derivatives have been identified as GPBAR1 agonists, however their clinical application is hampered by the lack of selectivity toward the other bile acid receptors. Therefore, non-steroidal GPBAR1 ligands able to selectively activate the receptor are urgently needed. With this aim, we here designed, synthesized and biologically evaluated ((1,2,4-oxadiazol-5-yl)pyrrolidin-3-yl) urea derivatives as novel potent GPBAR1 agonists. Particularly, compounds 9 and 10 induce the mRNA expression of the GPBAR1 target gene pro-glucagon and show high selectivity over the other bile acid receptors FXR, LXRα, LXRβ and PXR, and the related receptors PPARα and PPARγ. Computational studies elucidated the binding mode of 10 to GPBAR1, providing important structural insights for the design of non-steroidal GPBAR1 agonists. The pharmacokinetic properties of 9 and 10 suggest that the ((1,2,4-oxadiazol-5-yl)pyrrolidin-3-yl)ureydil scaffold might be exploited to achieve effective drug candidates to treat GPBAR1 related disorders.
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