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

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.

Graphical abstractThe importance of R1 substitution and orientation was studied. The (d) Trp residue as starting material was found to lead to the best agonist or antagonist compounds.Figure optionsDownload full-size imageDownload as PowerPoint slide