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Bioorg Med Chem ; 20(12): 3719-27, 2012 Jun 15.
Artículo en Inglés | MEDLINE | ID: mdl-22609074

RESUMEN

In this study thirty-three novel indole derivatives were designed and synthesized based on the structure of deformylflustrabromine B (1), a metabolite isolated from the marine bryozoan Flustra foliacea L. The syntheses were carried out using standard methodologies and in good yields. The molecules were tested for their affinities for the α4ß2(∗), α3ß4(∗), α7(∗) and (α1)(2)ß1γδ nicotinic acetylcholine receptor (nAChR) subtypes. Binding assays showed that, among these ligands, compound 7c exhibited the highest affinity with K(i)=136.1, 93.9 and 862.4nM for the α4ß2(∗), α3ß4(∗), and α7(∗) nAChRs subtypes, respectively. These results indicated that the indole core might be a useful scaffold for the development of new potent and selective nAChR ligands.


Asunto(s)
Indoles/síntesis química , Indoles/farmacología , Compuestos de Amonio Cuaternario/síntesis química , Compuestos de Amonio Cuaternario/farmacología , Receptores Nicotínicos/metabolismo , Animales , Briozoos/química , Bovinos , Indoles/química , Ligandos , Estructura Molecular , Compuestos de Amonio Cuaternario/química , Ratas , Relación Estructura-Actividad
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