- TUNABLE PHENYLACETYLENE HOSTS
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A compound, or a salt thereof, having the formula wherein Y is n is 1 or 2; each R is independently H, alkyl, substituted alkyl, a polyether moiety, carboxyl, substituted carboxyl, carbamate, substituted carbonate, carbonyloxy, alkoxy, substituted alkoxy,
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- New prodrugs of Adefovir and Cidofovir
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New Adefovir (PMEA) prodrugs with a pro-moiety consisting of decyl or decyloxyethyl chain bearing hydroxyl function(s), hexaethyleneglycol or a (5-methyl-2-oxo-1,3-dioxolen-4-yl)methyl unit were prepared starting from the tetrabutylammonium salt of the phosphonate drug and an appropriate alkyl bromide or tosylate. Analogously, two esters of Cidofovir [(S)-HPMPC] bearing a hexaethyleneglycol moiety were prepared. The activity of the prodrugs was evaluated in vitro against different virus families. A loss in the antiviral activities of the hydroxylated decyl or decyloxyethyl esters and hexaethyleneglycol esters of PMEA against human immunodeficiency virus (HIV) and herpesviruses [including herpes simplex virus (HSV), varicella-zoster virus (VZV), and human cytomegalovirus (CMV)] occurred in comparison with the parent compound. On the other hand, the (5-methyl-2-oxo-1,3-dioxolen-4-yl)methyl ester of PMEA showed significant activities against HIV and herpesviruses. (S)-HPMPC prodrugs exhibited anti-cytomegalovirus activities in the same range as the parent drug, whereas the anti-HSV and anti-VZV activities were one- to seven-fold lower than that of Cidofovir.
- Tichy, Tomá?,Andrei, Graciela,Dra?ínsky, Martin,Holy, Antonín,Balzarini, Jan,Snoeck, Robert,Kre?merová, Marcela
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experimental part
p. 3527 - 3539
(2011/07/09)
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- Supramolecular formation of fibrous nanostructure in donor-acceptor dyad film
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A novel oligothiophene and its fullerene derivative were synthesized and their film morphologies were investigated. AFM images revealed that the oligothiophene formed well-aligned fiber-like nanostructures in the film after being thermally annealed at its liquid-crystalline temperature. In the oligothiophene-fullerene dyad film, fibers were already formed in the as-cast film. Thermal annealing further enhanced the structural order and a long, partially aligned fibrous nanostructure with a width of around 10 nm and a length of as long as 200 nm was observed. Combined with the results of X-ray analysis, these features were ascribed to supramolecular self-assembly via π-π interaction of the oligothiophene groups. Photovoltaic properties of the molecules were also investigated. The Royal Society of Chemistry.
- Nishizawa, Takeshi,Tajima, Keisuke,Hashimoto, Kazuhito
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p. 2440 - 2445
(2008/09/21)
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- A chemoselective approach to grafting biodegradable polyesters
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The process of chemoselective coupling applied to side chains of poly(ethylene oxide) (PEO) grafted to ketone-bearing polyetsers yielding biodegradable polyesters, was investigated. Chemoselective coupling was performed by mixing the ketone-bearing PCL an
- Taniguchi, Ikuo,Mayes, Anne M.,Chan, Eugene W. L.,Griffith, Linda G.
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p. 216 - 219
(2007/10/03)
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- Multigram Synthesis of Well-Defined Extended Bifunctional Polyethylene Glycol (PEG) Chains
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A series of novel, well-defined, unsymmetrical poly(ethylene glycol) chains of the type X(OCH2-CH2)nY (where X = protecting group; Y = nucleofuge or a different protecting group; n = 3, 6, 9, 12, 15, 18, and 24) were prepared in high yields by applying orthogonal protecting groups. The purity of the compounds was fully verified by elemental and high-resolution mass spectrometry analyses.
- Loiseau, Francois A.,Hii, King Kuok,Hill, Alison M.
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p. 639 - 647
(2007/10/03)
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- Synthesis of heparin-like antithrombotics having perphosphorylated thrombin binding domains
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The synthesis of three heparin analogues (i.e. compounds VI-VIII) having perphosphorylated thrombin binding domains (TBDs) is reported. These compounds were tested in vitro for their antithrombin III (ATIII)-mediated anti-Xa and antithrombin activities. Conjugates VI and VIII show a remarkable increase in antithrombin activity compared to the structurally related conjugates with persulfated TBDs (i.e. compounds IV and V), whereas compound VII displays a diminished activity.
- Buijsman, Rogier C.,Basten, Jan E. M.,Dreef-Tromp, Cornelia M.,Van Der Marel, Gijsbert A.,Van Boeckel, Constant A. A.,Van Boom, Jacques H.
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p. 1881 - 1890
(2007/10/03)
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