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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
Authors: Ceras, J. (Javier)
Cirauqui, N. (Nuria)
Perez-Silanes, S. (Silvia)
Aldana, I. (Ignacio)
Monge, A. (Antonio)
Galiano, S. (Silvia)
Keywords: Histamine H3 receptor
Type 2 diabetes mellitus
Issue Date: 2012
Publisher: Elsevier
Publisher version:
ISSN: 0223-5234
Citation: 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.
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.
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Appears in Collections:DA - Farmacia - Orgánica - Artículos de revista
DA - CIFA - I+D de medicamentos - Artículos de revistas

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