674819-29-5Relevant academic research and scientific papers
Synthesis of new thiophene and benzo[b]thiophene hydrazide derivatives as human NPY Y5 antagonists
Galiano, Silvia,Erviti, Oihana,Perez, Silvia,Moreno, Antonio,Juanenea, Laura,Aldana, Ignacio,Monge, Antonio
, p. 597 - 599 (2004)
Neuropeptide Y is one of the most potent appetite stimulating hormones known. Novel thiophene and benzo[b]thiophene hydrazide derivatives were synthetized and evaluated biologically as NPY Y1 and Y5 receptor subtype antagonists. They were found to have nanomolar binding affinities for human NPY Y5 receptor, obtaining the lead compound, trans-N-4-[N′-(thiophene-2-carbonyl)hydrazinocarbonyl]cyclohexylmethyl-4- bromobenzenesulfonamide, which binds with a 7.70 nM IC50 to the hY5 receptor.
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
