5045-94-3Relevant academic research and scientific papers
Multivalent agents containing 1-substituted 2,3,4-trihydroxyphenyl moieties as novel synthetic polyphenols directed against HIV-1
Flores, Aida,Camarasa, Maria Jose,Perez-Perez, Maria Jesus,San-Felix, Ana,Balzarini, Jan,Quesada, Ernesto
, p. 5278 - 5294 (2014/07/08)
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.
Improved synthesis of an ethereal tetraamine core for dendrimer construction
Newkome, George R.,Mishra, Amaresh,Moorefield, Charles N.
, p. 3957 - 3960 (2007/10/03)
A new route to a pentaerythritol-based tetra-amine is delineated and subsequently contrasted to a previous report. Access to the pure tetraamine is facilitated by the smooth reduction of its tetraazide precusor. Characterization includes the preparation of a 4:1 Zn-tetraphenylporphyrin/tetraamine complex.
