New Derivatives of 5-Substituted Uracils: Potential Agents with a Wide Spectrum of Biological Activity

Pyrimidine nucleoside analogues are widely used to treat infections caused by the human immunodeficiency virus (HIV) and DNA viruses from the herpes family. It has been shown that 5-substituted uracil derivatives can inhibit HIV-1, herpes family viruses, mycobacteria and other pathogens through various mechanisms. Among the 5-substituted pyrimidine nucleosides, there are not only the classical nucleoside inhibitors of the herpes family viruses, 2′-deoxy-5-iodocytidine and 5-bromovinyl-2′-deoxyuridine, but also derivatives of 1-(benzyl)-5-(phenylamino)uracil, which proved to be non-nucleoside inhibitors of HIV-1 and EBV. It made this modification of nucleoside analogues very promising in connection with the emergence of new viruses and the crisis of drug resistance when the task of creating effective antiviral agents of new types that act on other targets or exhibit activity by other mechanisms is very urgent. In this paper, we present the design, synthesis and primary screening of the biological activity of new nucleoside analogues, namely, 5′-norcarbocyclic derivatives of substituted 5-arylamino- and 5-aryloxyuracils, against RNA viruses.     

New Cysteine-Containing PEG-Glycerolipid Increases the Bloodstream Circulation Time of Upconverting Nanoparticles

Upconverting nanoparticles have unique spectral and photophysical properties that make them suitable for development of theranostics for imaging and treating large and deep-seated tumors. Nanoparticles based on NaYF₄ crystals doped with lanthanides Yb³⁺ and Er³⁺ were obtained by the high-temperature decomposition of trifluoroacetates in oleic acid and 1-octadecene. Such particles have pronounced hydrophobic properties. Therefore, to obtain stable dispersions in aqueous media for the study of their properties in vivo and in vitro, the polyethylene glycol (PEG)-glycerolipids of various structures were obtained. To increase the circulation time of PEG-lipid coated nanoparticles in the bloodstream, long-chain substituents are needed to be attached to the glycerol backbone using ether bonds. To prevent nanoparticle aggregation, an L-cysteine-derived negatively charged carboxy group should be included in the lipid molecule.     

THE EFFECT OF ALCOHOLS WITH DIFFERENT STRUCTURES ON THE FORMATION OF WARM O/W MICROEMULSIONS

The influence of twenty five different alcohols on the formation of warm oil-in-water (O/W) microemulsions was investigated. Selected concentrations of each alcohol were added to fixed amounts of stearic acid, Tween 20 and water at 65 ° C. Fifteen alcohols formed microemulsions, at least at one of the concentrations. A pattern recognition study was performed to elucidate the activities of the alcohols by Principal Component Analysis (PCA). Linear Discriminant Analysis (LDA) was used to classify them. Two classification functions, obtained for alcohols forming / not forming microemulsions, suggest that the formation of warm O/W microemulsion is linked to the nature and the dimension/lipophilicity of the alcohol.     

DIE AMBIDENTE REAKTIONSFÄHIGKEIT DES RHODANIDANIONS IN DER REAKTION MIT 2-PROPOXYCARBONYLTHIOCYANAT

Abstract

By pursuing the reaction between 2-propyloxycarbonylthiocyanate and ¹⁴C-potassiumrhodanide the relative reactivity of the nitrogen and sulfur in the rhodanideanion has been determined.

Durch Verfolgen der Reaktion zwischen 2-Propoxycarbonylthiocyanat und ¹⁴C markiertem Kaliumrh odanid wurde die relative Reaktionsfähigkeit des Rhodanidanions in bezug auf das Stickstoffatom und das Schwefelatom bestimmt.     

Kinetics of homogeneous dehydrogenation of formic acid in the presence of supramolecular rhodium(III) complex with P-functionalized calix[4]resorcine

The kinetics of homogeneous dehydrogenation of formic acid in the presence of supramolecular rhodium(III) complex with P-functionalized calix[4]resorcine were studied in dioxane, tetrahydrofuran, dimethylformamide, and binary formamide-dioxane mixtures (volume ratio 10: 90, 20: 80, 30: 70) over a wide temperature range (40?C90°C). The examined Rh(III) complex catalyzed the dehydrogenation process, and its catalytic activity was higher than that observed previously for rhodium complexes with non-macrocyclic phosphorus-containing ligands. The dehydrogenation rate constants were proportional to neither catalyst concentration nor dielectric constant of the medium, which is likely to be related to supramolecular nature of the Rh(III) complex. No micelle formation was observed in the examined systems.     

Unexpected formation of dinaphthoaza-17-crown-5 ether containing γ-aminopiperidine subunit

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An efficient synthesis of new polyfunctional hexahydro pyrido[1,2-a]pyrazin-1-ones

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Electrochemical performance of lithium titanate anode fabricated using a water-based binder

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