The 21-amino acid peptide endothelin-1 (ET-1) is the predominant isoform of the endothelin peptide family,which includes ET-2, and ET-3. These peptides display a variety of physiological activities including vasoconstriction andthe stimulation of cell proliferation in tissues both within and outside of the cardiovascular system. They exert their actionsvia activation of two distinct receptor subtypes, ETA and ETB, belonging to the G protein-coupled receptor (GPCR) superfamily.Ligands of these receptors have received numerous citations in the recent pharmaceutical literature. In particularreceptor antagonists, both ETA- and ETB-selective, as well as non-selective, have been described due to their wide therapeuticpotential. As a part of our program toward the development of selective ETA ligands we have designed and we nowreport new molecules based on 2-substituted-4-aryl-3-quinolinecarboxylic acid moiety. Binding profile for some compounds(40, 44, 46, and 47) of this class showed a reasonable affinity and selectivity for ETA receptors.
|Titolo:||Synthesis and Endothelin Receptor Binding Affinity of a Novel Class of 2-Substituted-4-aryl-3-quinolinecarboxylic Acid Derivatives|
|Data di pubblicazione:||2008|
|Appare nelle tipologie:||1.1 Articolo in rivista|