N. S. Shastina

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The inhibitors of viral adsorption are a new generation of antiviral drugs, which can be used in the therapy of HIV infection. The review presents different classes of the HIV entry inhibitors, which are grouped according to the processes they are targeting: the interaction of the viral glycoprotein gp120 with the cell receptor CD4, the secondary(More)
The total synthesis of 1(3)-O-(rac-1,2-dipalmitoylglycerophospho)-4(6)-O- beta-D-glucopyranosyl-sn-myo-inositol was performed. The major stages of the synthetic route are glycosylation of the substituted myo-inositol derivative by the glycosyl fluoride method and creation of the phosphorus moiety of the target glycolipid by means of the H-phosphonate(More)
Methods for producing prothrombin complex concentrate (PPSB) by anion-exchange chromatography in batch mode using various sorbents such as DEAE- and QAE-Sephadex A-50 were examined. It was established that the yield and specific activity of FII, FVII, FIX, and FX depended on the mass of resin used for chromatography. New column chromatography methods for(More)
A partially protected phosphatidylinositol with a free hydroxyl group in the cyclitol moiety was synthesized by phosphorylation of a tetrasubstituted myo-inositol using the H-phosphonate and phosphoamidite methods. The H-phosphonate method was advantageous for the synthesis of selectively protected monophosphoinositide due to a lesser number of stages. Two(More)
For the purpose of finding effective inhibitors of virus adsorption the series of inositol-containing phospholipid dimer analogues were previously synthesized. In the present work, the antiretroviral activity of these compounds against HIV-1 was demonstrated on the model of cells infected with the virus. The highest effect was found in the case of dimer(More)
One of the approaches to enhance the bioavailability of nucleoside reverse transcriptase HIV inhibitors is the design of their prodrugs based on 1,3-diacylglycerols, which may simulate metabolic pathways of natural lipids, thus supporting the efficacy of drug delivery to the target cells. Glycerolipid AZT conjugates with different functional phosphoric(More)
Synthesis of anti-HIV nucleoside lipophilic derivatives with diol compounds in which two antiviral pharmacophore residues are linked by a single hydrophobic fragment is described. It is suggested to use 2,3,4,5-tetra-O-benzyl-D, L-iditol and 1,12-dodecanediol as hydrophobic transport systems. Succinic and phosphodiester fragments were used for binding(More)
The search for new, effective antiviral agents currently includes assessment of polyanionic compounds of various structures; these are highly active inhibitors of viral penetration into cells. The present report describes the preparation of phosphate and sulfate derivatives based on 2,3,4,5-tetra-O-benzyl-D,L-iditol, 1,12-dodecanediol, and a dimeric analog(More)
A partially protected phosphatidylinositol with a free hydroxyl group in the cyclitol moiety was synthesized by phosphorylation of a tetrasubstituted myo-inositol using the H-phosphonate and phosphoamidite methods. The H-phosphonate method was advantageous for the synthesis of selectively protected monophosphoinositide due to a lesser number of stages. Two(More)
A promising approach to enhancing the bioavailability of hydrophilic therapeutic agents including anti-HIV nucleosides is designing their pseudotriglyceride derivatives that may mimic natural lipids and take advantage of their metabolic pathways resulting in improved delivery to target cells. The synthesis of a series of new 1,3-diglycerides and AZT(More)