Trisubstituted 1,2,4-triazoles as ligands for the ghrelin receptor: On the significance of the orientation and substitution at position 3

Aline Moulin, Luc Demange, Joanne Ryan, Céline M'Kadmi, Jean Claude Galleyrand, Jean Martinez, Jean Alain Fehrentz

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18 Citations (Scopus)

Abstract

The synthesis and structure-activity relationships concerning 3,4,5-trisubstituted 1,2,4-triazoles as ghrelin receptor ligands are described. The importance of the starting aminoacid material as well as its configuration was explored and the (d) Trp residue was found to lead to the best agonist or antagonist compounds.

Original languageEnglish
Pages (from-to)164-168
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume18
Issue number1
DOIs
Publication statusPublished - 1 Jan 2008
Externally publishedYes

Keywords

  • 1,2,4-Triazole
  • Agonist
  • Antagonist
  • Ghrelin
  • Ghrelin receptor ligands
  • GHS-R1a
  • Trisubstituted 1,2,4-Triazoles

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