Abstract
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 and the stimulation of cell proliferation in tissues both within and outside of the cardiovascular system. They exert their actions via 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 particular receptor antagonists, both ETA- and ETB-selective, as well as non-selective, have been described due to their wide therapeutic potential. As a part of our program toward the development of selective ETA ligands we have designed and we now report 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.
Keywords: 2-Substituted-4-aryl-3-quinolinecarboxylic acids derivatives, endothelin receptors, G protein-coupled receptors, hypertension
Medicinal Chemistry
Title: Synthesis and Endothelin Receptor Binding Affinity of a Novel Class of 2-Substituted-4-aryl-3-quinolinecarboxylic Acid Derivatives
Volume: 4 Issue: 2
Author(s): Valeria Pittala, Maria Modica, Loredana Salerno, Maria Angela Siracusa, Francesco Guerrera, Ilario Mereghetti, Alfredo Cagnotto, Tiziana Mennini and Giuseppe Romeo
Affiliation:
Keywords: 2-Substituted-4-aryl-3-quinolinecarboxylic acids derivatives, endothelin receptors, G protein-coupled receptors, hypertension
Abstract: 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 and the stimulation of cell proliferation in tissues both within and outside of the cardiovascular system. They exert their actions via 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 particular receptor antagonists, both ETA- and ETB-selective, as well as non-selective, have been described due to their wide therapeutic potential. As a part of our program toward the development of selective ETA ligands we have designed and we now report 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.
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Cite this article as:
Pittala Valeria, Modica Maria, Salerno Loredana, Siracusa Angela Maria, Guerrera Francesco, Mereghetti Ilario, Cagnotto Alfredo, Mennini Tiziana and Romeo Giuseppe, Synthesis and Endothelin Receptor Binding Affinity of a Novel Class of 2-Substituted-4-aryl-3-quinolinecarboxylic Acid Derivatives, Medicinal Chemistry 2008; 4 (2) . https://dx.doi.org/10.2174/157340608783789095
DOI https://dx.doi.org/10.2174/157340608783789095 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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