Synthesis and endothelin receptor binding affinity of a novel class of 2-substituted-4-aryl-3-quinolinecarboxylic acid derivatives

Valeria Pittalà, Maria Modica, Loredana Salerno, Maria Angela Siracusa, Francesco Guerrera, Ilario Mereghetti, Alfredo Cagnotto, Tiziana Mennini, Giuseppe Romeo

Research output: Contribution to journalArticlepeer-review

Abstract

The 21-amino acid peptide endothelin-1 (ET-1) is the predominant isoform of the endothelin peptide family, which incrdes 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) super-family. 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.

Original languageEnglish
Pages (from-to)129-137
Number of pages9
JournalMedicinal Chemistry
Volume4
Issue number2
DOIs
Publication statusPublished - Mar 2008

Keywords

  • 2-Substituted-4-aryl-3-quinolinecarboxylic acids derivatives
  • Endothelin receptors
  • G. protein-coupled receptors
  • Hypertension

ASJC Scopus subject areas

  • Drug Discovery

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