The synthesis of seventeen new 1,3-diaryl-5-oxo-proline derivatives as endothelin receptor (ETR) ligands is described. The structural configuration of the new molecules was determined by analyzing selected signals in proton NMR spectra. In vitro binding assays of the human ET and ET receptors allowed us to identify compound as a selective ETR ligand. The molecular docking of the selected compounds and the ET antagonist atrasentan in the ETR homology model provided insight into the structural elements required for the affinity and the selectivity of the ETR subtype.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7221592 | PMC |
| http://dx.doi.org/10.3390/molecules25081851 | DOI Listing |
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