247936-90-9Relevant academic research and scientific papers
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.
Synthesis and evaluation of new hydrazide derivatives as neuropeptide Y Y5 receptor antagonists for the treatment of obesity
Juanenea, Laura,Galiano, Silvia,Erviti, Oihana,Moreno, Antonio,Pérez, Silvia,Aldana, Ignacio,Monge, Antonio
, p. 4717 - 4723 (2007/10/03)
NPY is the most potent orexigenic agent known to man, with NPY Y1 and NPY Y5 being the receptor subtypes that are most likely responsible for centrally-mediated NPY-induced feeding responses. Based on the aforementioned, novel hydrazide derivatives were prepared for the purpose of searching new NPY Y5 receptor antagonists. Many of the compounds exhibited nanomolar binding affinity for this receptor, affording trans-N-{4-[N′-(3,4-dichlorophenyl) hydrazinocarbonyl]cyclohexylmethyl}-4-fluorobenzenesulfonamide, which showed the best activity (IC50=0.43 nM). NPY is the most potent orexigenic agent known to man, with NPY Y1 and NPY Y5 being the receptor subtypes that are most likely responsible for centrally-mediated NPY-induced feeding responses. Based on the aforementioned, novel hydrazide derivatives were prepared for the purpose of searching new NPY Y5 receptor antagonists. Many of the compounds exhibited nanomolar binding affinity for this receptor, affording trans-N-{4-[N′-(3,4-dichlorophenyl)hydrazinocarbonyl]cyclohexylmethyl} -4-fluorobenzenesulfonamide, which showed the best activity (IC 50=0.43 nM).
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 (2007/10/03)
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.
SUBSTITUTED 2-CYCLOHEXYL-4-PHENYL-1H-IMIDAZOLE DERIVATIVES
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, (2008/06/13)
Substituted 2-cyclohexyl-4-phenyl-1H-imidazole derivatives capable of modulating NPY5 receptor activity, are provided. Such compounds may be used to modulate NPY binding to NPY5 receptors in vivo or in vitro, and are particularly useful in the treatment o
Novel histone deacetylase inhibitors: N-hydroxycarboxamides possessing a terminal bicyclic aryl group
Uesato, Shinichi,Kitagawa, Manabu,Nagaoka, Yasuo,Maeda, Taishi,Kuwajima, Hiroshi,Yamori, Takao
, p. 1347 - 1349 (2007/10/03)
Utilizing tranexamic acid as a starting material, a series of N-hydroxycarboxamides were synthesized in order to seek new histone deacetylase (HDAC) inhibitors. Further structure optimization involving the replacement of the 1,4-cyclohexylene group with t
