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.
Moulin
Aline
A
Institut des Biomolécules Max Mousseron, UMR 5247, CNRS-Université Montpellier I, BP 14491, Faculté de Pharmacie, 15 avenue Charles Flahault, 34093 Montpellier Cedex 5, France.
Demange
Luc
L
Ryan
Joanne
J
M'Kadmi
Céline
C
Galleyrand
Jean-Claude
JC
Martinez
Jean
J
Fehrentz
Jean-Alain
JA
D008024:Ligands; D054440:Receptors, Ghrelin / Q000819:agonists / Q000037:antagonists & inhibitors / Q000737:chemistry* / Q000378:metabolism; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology
D008024:Ligands; D054440:Receptors, Ghrelin; D014230:Triazoles