Por favor, use este identificador para citar o enlazar a este item:
http://hdl.handle.net/10261/100972
COMPARTIR / EXPORTAR:
SHARE CORE BASE | |
Visualizar otros formatos: MARC | Dublin Core | RDF | ORE | MODS | METS | DIDL | DATACITE | |
Título: | Multivalent agents containing 1-substituted 2,3,4-trihydroxyphenyl moieties as novel synthetic polyphenols directed against HIV-1 |
Autor: | Flores, Aida CSIC; Camarasa Rius, María José CSIC ORCID; Peréz-Pérez, María-Jesús CSIC ORCID ; San-Félix, Ana CSIC ORCID ; Balzarini, Jan; Quesada, Ernesto CSIC ORCID | Fecha de publicación: | 2014 | Editor: | Royal Society of Chemistry (UK) | Citación: | Organic and Biomolecular Chemistry 12: 5278-5294 (2014) | Resumen: | The synthesis and the assessment of the anti-HIV activity of a set of molecules inspired by the multivalent structures of some naturally-occurring polyphenols (tannins) are reported. Different multibranched scaffolds have been derived from pentaerythritol as the central core which distribute spatially synthetic polyphenolic subunits based on 1-substituted 2,3,4-trihydroxyphenyl moieties. A tetrapodal compound (13b) bearing four N-(2,3,4-trihydroxyphenyl) amide groups, exhibits remarkable selective activity against HIV-1 with EC 50 values in the micromolar scale, in the same range as those reported for the most representative anti-HIV tannins. Preliminary SAR studies emphasize the importance of the 1-substituted 2,3,4-trihydroxyphenyl moiety, the presence of an amide as the linker and the multivalent architecture of these molecules, since the anti-HIV activity increases with the number of polyphenolic moieties. The data support the interest in synthetic polyphenols and represent a promising starting point for further design and development of selective HIV-1 inhibitors. | Versión del editor: | http://dx.doi.org/10.1039/c4ob00445k | URI: | http://hdl.handle.net/10261/100972 | DOI: | 10.1039/c4ob00445k | Identificadores: | doi: 10.1039/c4ob00445k issn: 1477-0520 e-issn: 1477-0539 |
Aparece en las colecciones: | (IQM) Artículos |
Ficheros en este ítem:
Fichero | Descripción | Tamaño | Formato | |
---|---|---|---|---|
Org. Biomol. Chem., 2014.pdf | 4,24 MB | Adobe PDF | Visualizar/Abrir |
CORE Recommender
SCOPUSTM
Citations
13
checked on 18-abr-2024
WEB OF SCIENCETM
Citations
13
checked on 25-feb-2024
Page view(s)
274
checked on 18-abr-2024
Download(s)
424
checked on 18-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.