Por favor, use este identificador para citar o enlazar a este item:
http://hdl.handle.net/10261/123461COMPARTIR / EXPORTAR:
 SHARE
 CORE
BASE
|
|
| Visualizar otros formatos: MARC | Dublin Core | RDF | ORE | MODS | METS | DIDL | DATACITE | |
| Título: | Novel N-acetyl bioisosteres of melatonin: Melatonergic receptor pharmacology, physicochemical studies, and phenotypic assessment of their neurogenic potential |
Autor: | Fuente Revenga, Mario de la CSIC ORCID; Fernández-Sáez, Nerea CSIC; Herrera-Arozamena, Clara CSIC ORCID CVN; Morales-García, José A. CSIC ORCID; Alonso-Gil, Sandra CSIC; Pérez Castillo, Ana CSIC ORCID; Caignard, Daniel-Henri; Rivara, Silvia; Rodríguez-Franco, María Isabel CSIC ORCID | Fecha de publicación: | 2015 | Editor: | American Chemical Society | Citación: | Journal of Medicinal Chemistry 58(12): 4998-5014 (2015) | Resumen: | Herein we present a new family of melatonin-based compounds, in which the acetamido group of melatonin has been bioisosterically replaced by a series of reversed amides and azoles, such as oxazole, 1,2,4-oxadiazole, and 1,3,4-oxadiazole, as well as other related five-membered heterocycles, namely, 1,3,4-oxadiazol(thio)ones, 1,3,4-triazol(thio)ones, and an 1,3,4-thiadiazole. New compounds were fully characterized at melatonin receptors (MT<inf>1</inf>R and MT<inf>2</inf>R), and results were rationalized by superimposition studies of their structures to the bioactive conformation of melatonin. We also found that several of these melatonin-based compounds promoted differentiation of rat neural stem cells to a neuronal phenotype in vitro, in some cases to a higher extent than melatonin. This unique profile constitutes the starting point for further pharmacological studies to assess the mechanistic pathways and the relevance of neurogenesis induced by melatonin-related structures. | Descripción: | et al. | URI: | http://hdl.handle.net/10261/123461 | DOI: | 10.1021/acs.jmedchem.5b00245 | Identificadores: | doi: 10.1021/acs.jmedchem.5b00245 issn: 0022-2623 e-issn: 1520-4804 |
| Aparece en las colecciones: | (IQM) Artículos (IIBM) Artículos |
Ficheros en este ítem:
| Fichero | Descripción | Tamaño | Formato | |
|---|---|---|---|---|
| accesoRestringido.pdf | 15,38 kB | Adobe PDF |  Visualizar/Abrir |
CORE Recommender
SCOPUSTM
Citations
36
checked on 20-abr-2024
WEB OF SCIENCETM
Citations
34
checked on 25-feb-2024
Page view(s)
239
checked on 20-abr-2024
Download(s)
141
checked on 20-abr-2024
Google ScholarTM
Check
Altmetric
Altmetric
NOTA: Los ítems de Digital.CSIC están protegidos por copyright, con todos los derechos reservados, a menos que se indique lo contrario.