- Combining NMR and molecular modelling in a drug delivery context: Investigation of the multi-mode inclusion of a new NPY-5 antagonist bromobenzenesulfonamide into β-cyclodextrin
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NMR spectroscopic and molecular modelling methods have been employed to describe the complexation of trans-N-4-[N′-(4-chlorobenzoyl) hydrazinocarbonyl]cyclohexylmethyl-4-bromobenzenesulfonamide, a new chemotype of NPY-5 antagonist, and β-cyclodextrin, rev
- Uccello-Barretta, Gloria,Balzano, Federica,Sicoli, Giuseppe,Friglola, Carmen,Aldana, Ignacio,Monge, Antonio,Paolino, Donatella,Guccione, Salvatore
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- Synthesis and description of intermolecular interactions in new sulfonamide derivatives of tranexamic acid
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Tranexamic acid (4-aminomethyl-cyclohexanecarboxylic acid) was reacted with sulfonyl chlorides to produce structurally related four sulfonamide derivatives using simple and environmental friendly method to check out their three-dimensional behavior and va
- Ashfaq, Muhammad,Arshad, Muhammad Nadeem,Danish, Muhammad,Asiri, Abdullah M.,Khatoon, Sadia,Mustafa, Ghulam,Zolotarev, Pavel N.,Butt, Rabia Ayub,?ahin, Onur
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p. 271 - 280
(2015/10/19)
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- Novel human neuropeptide Y Y5 receptor antagonists for the treatment of obesity: Synthesis and biological evaluation of pyridine hydrazide derivatives
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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
- Galiano, Silvia,Erviti, Oihana,Perez, Silvia,Moreno, Antonio,Juanenea, Laura,Aldana, Ignacio,Monge, Antonio
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- Synthesis of new thiophene and benzo[b]thiophene hydrazide derivatives as human NPY Y5 antagonists
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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.
- Galiano, Silvia,Erviti, Oihana,Perez, Silvia,Moreno, Antonio,Juanenea, Laura,Aldana, Ignacio,Monge, Antonio
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p. 597 - 599
(2007/10/03)
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- Synthesis and evaluation of new arylsulfonamidomethylcyclohexyl derivatives as human neuropeptide Y Y 5 receptor antagonists for the treatment of obesity
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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.
- Moreno, Antonio,Perez, Silvia,Galiano, Silvia,Juanenea, Laura,Erviti, Oihana,Frigola, Carmen,Aldana, Ignacio,Monge, Antonio
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- Synthesis and evaluation of new hydrazide derivatives as neuropeptide Y Y5 receptor antagonists for the treatment of obesity
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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).
- Juanenea, Laura,Galiano, Silvia,Erviti, Oihana,Moreno, Antonio,Pérez, Silvia,Aldana, Ignacio,Monge, Antonio
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p. 4717 - 4723
(2007/10/03)
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