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Dadun > Depósito Académico > CIFA (Centro de Investigación en Farmacobiología Aplicada) > Unidad de I+D de Medicamentos > DA - CIFA - I+D de medicamentos - Artículos de revistas >

Novel sulfonylurea derivatives as H3 receptor antagonists. Preliminary SAR studies
Autor(es) : Ceras, J. (Javier)
Cirauqui, N. (Nuria)
Perez-Silanes, S. (Silvia)
Aldana, I. (Ignacio)
Monge, A. (Antonio)
Galiano, S. (Silvia)
Palabras clave : Histamine H3 receptor
Obesity
Sulfonylurea
Type 2 diabetes mellitus
Fecha incorporación: 2012
Editorial : Elsevier
Versión del editor: http://dx.doi.org/10.1016/j.ejmech.2012.02.049
ISSN: 0223-5234
Cita: Ceras J, Cirauqui N, Pérez-Silanes S, Aldana I, Monge A, Galiano S. Novel sulfonylurea derivatives as H3 receptor antagonists. Preliminary SAR studies. Eur J Med Chem 2012 6;52(0):1-13.
Resumen
The combination of antagonism at histamine H3 receptor and the stimulation of insulin secretion have been proposed as an approach to new dual therapeutic agents for the treatment of type 2 diabetes mellitus associated with obesity. We have designed and synthesized a new series of non-imidazole derivatives, based on a basic amine ring connected through an alkyl spacer of variable length to a phenoxysulfonylurea moiety. These compounds were initially evaluated for histamine H3 receptor binding affinities, suggesting that a propoxy chain linker between the amine and the core ring could be essential for optimal binding affinity. Compound 56, 1-(naphthalen-1-yl)-3-[(p-(3-pyrrolidin-1-ylpropoxy)benzene)]sulfonylurea exhibited the best H3 antagonism affinity. However, since all these derivatives failed to block KATP channels, the link of these two related moieties should not be considered a good pharmacophore for obtaining new dual H3 antagonists with insulinotropic activity, suggesting the necessity to propose a new chemical hybrid prototype.
Enlace permanente: http://hdl.handle.net/10171/23595
Aparece en las colecciones: DA - Farmacia - Orgánica - Artículos de revista
DA - CIFA - I+D de medicamentos - Artículos de revistas

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Fichero:  EJMC 2012 (J. Ceras).pdf
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