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Multivalent agents containing 1-substituted 2,3,4-trihydroxyphenyl moieties as novel synthetic polyphenols directed against HIV-1

AuthorsFlores, Aida ; Camarasa Rius, María José ; Peréz-Pérez, María-Jesús ; San-Félix, Ana ; Balzarini, Jan; Quesada, Ernesto
Issue Date2014
PublisherRoyal Society of Chemistry (UK)
CitationOrganic and Biomolecular Chemistry 12: 5278-5294 (2014)
AbstractThe 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.
Publisher version (URL)http://dx.doi.org/10.1039/c4ob00445k
Identifiersdoi: 10.1039/c4ob00445k
issn: 1477-0520
e-issn: 1477-0539
Appears in Collections:(IQM) Artículos
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