The synthesis of seventeen new 1,3-diaryl-5-oxo-proline derivatives as endothelin receptor\n(ETR) ligands is described. The structural configuration of the new molecules was determined by\nanalyzing selected signals in proton NMR spectra. In vitro binding assays of the human ETA and ETB\nreceptors allowed us to identify compound 31h as a selective ETAR ligand. The molecular docking of\nthe selected compounds and the ETA antagonist atrasentan in the ETAR homology model provided\ninsight into the structural elements required for the anity and the selectivity of the ETAR subtype.
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