691887-07-7Relevant academic research and scientific papers
Novel human neuropeptide Y Y5 receptor antagonists for the treatment of obesity: Synthesis and biological evaluation of pyridine hydrazide derivatives
Galiano, Silvia,Erviti, Oihana,Perez, Silvia,Moreno, Antonio,Juanenea, Laura,Aldana, Ignacio,Monge, Antonio
, p. 81 - 85 (2007/10/03)
A series of new pyridine hydrazide derivatives with high and selective antagonist activity at the human neuropeptide Y Y5 receptor were developed. Introduction of electron-withdrawing groups into the arylsulfonamide rest, together with the 3-py
Synthesis and evaluation of new arylsulfonamidomethylcyclohexyl derivatives as human neuropeptide Y Y 5 receptor antagonists for the treatment of obesity
Moreno, Antonio,Perez, Silvia,Galiano, Silvia,Juanenea, Laura,Erviti, Oihana,Frigola, Carmen,Aldana, Ignacio,Monge, Antonio
, p. 49 - 58 (2007/10/03)
NPY is the most potent orexigenic peptide identified up to now. Stimulation of food intake is measured by the Y1 and Y5 receptor subtypes. In this study, the synthesis and evaluation of new arylsulfonamidomethylcyclohexyl derivatives are described as potential selective antagonists of the human NPY Y5 receptor. The SAR of these series was examined and the amide derivatives were the compounds that showed the best activities. trans-N-{4-[(Quinolin-3-yl)aminocarbonyl]cyclohexylmethyl}- 2,4-dichlorobenzenesulfonamide (42) bound to the human neuropeptide Y Y 5 receptor with a 2 nM IC50.
