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.     

A Review of the Dawn of Benchtop EPR Spectrometers—Innovation That Shaped the Future of This Technology

By the early 1980s, unique devices appeared in the USSR: a series of benchtop specialized EPR spectrometers. This equipment was quickly accepted not only in science but also in medicine and in many technical and economic areas including chemical industries and geologic exploration. The appearance of these devices was perceived as a salvation for the Soviet magnetic resonance (MR) scientific instrumentation by those who worked in the field of EPR spectroscopy in the USSR. (However, the program of MR scientific instrumentation ceased to exist along with the USSR a few years later). The Belarusian State University in Minsk was the center of these developments. At that moment and for many years afterwards, these devices were unique with no analogues in the worldwide EPR industry. They remained the only mass-produced MR spectrometers on the territory of the former USSR after its collapse. For the first time, based on archival materials, patents, and our personal memoirs, we describe the development of these EPR spectrometers and discuss the most original technical solutions and the scientific tasks solved with this equipment We also remember the participants of the work, showing the historical context of these events.     

Distribution of Platinum and Palladium between Dissolved,Nanoparticulate, and Microparticulate Fractions of Road Dust

Ageing processes of vehicle catalytic converters inevitably lead to the release of Pt and Pd into the environment, road dust being the main sink. Though Pt and Pd are contained in catalytic converters in nanoparticulate metallic form, under environmental conditions, they can be transformed into toxic dissolved species. In the present work, the distribution of Pt and Pd between dissolved, nanoparticulate, and microparticulate fractions of Moscow road dust is assessed. The total concentrations of Pt and Pd in dust vary in the ranges 9–142 ng (mean 35) and 155–456 (mean 235) ng g⁻¹, respectively. The nanoparticulate and dissolved species of Pt and Pd in dust were studied using single particle inductively coupled plasma mass spectrometry. The median sizes of nanoparticulate Pt and Pd were 7 and 13 nm, respectively. The nanoparticulate fraction of Pt and Pd in Moscow dust is only about 1.6–1.8%. The average contents of dissolved fraction of Pt and Pd are 10.4% and 4.1%, respectively. The major fractions of Pt and Pd (88–94%) in road dust are associated with microparticles. Although the microparticulate fractions of Pt and Pd are relatively stable, they may become dissolved under changing environmental conditions and, hence, transformed into toxic species.     

Nonuniform distribution of absorbed energy in high-resistance materials excited by an electron beam

Experimental results are presented on the changes in the optical characteristics of lithium fluoride induced by an electron beam with time-varying density and pulse energies close to the threshold for destruction of the material. The spatial distribution of color centers is investigated, especially near breakdown channels. Mechanisms for nonuniform accumulation of defects are discussed, along with the fundamental causes of the inhomogeneous energy distributions induced by the high-current electron beam. Concrete results of calculations of the field intensity distribution in LiF crystals during irradiation are presented, based on models of “uniform” and nonuniform charging of the sample. An abrupt increase in the electric field intensity is predicted near the breakdown channel. Zh. Tekh. Fiz. 68, 53–59 (April 1998)     

Two-phase model of hydrolysis kinetics and its applications to anaerobic degradation of particulate organic matter

The various equations of hydrolysis kinetics included into the generalized simulation model (METHANE) were tested on the anaerobic digestion of cellulose, sludge, and cattle manure. The good agreement between the model simulation results and experimental data was obtained. The Contois equation, taking into account a hydrolytic biomass, and the firstorder equation with respect to the particulate substrate only, were shown to be the approximations of two-phase hydrolysis kinetics.     

Novel 2-aminoimidazole-4-one complexes of copper(II) and cobalt(II): Synthesis,structural characterization and cytotoxicity

A series of 2-aminosubstituted (5Z)-3-phenyl-5-(pyridine-2-ylmethylene)-3,5-dihydro-4H-imidazole-4-ones (L) was prepared by the reaction of the corresponding 2-alkylthio-3,5-dihydro-4H-imidazole-4-ones with morpholine or piperidine in the presence of ytterbium(III) triflate. The resulting ligands were subsequently reacted with CuCl₂·2H₂O and CoCl₂·6H₂O to give the corresponding copper(II) and cobalt(II) complexes, respectively. Analysis revealed that the complexes were formed with an LMCl₂ (M = Cu, Co)-type composition in all cases. The structures of the three cobalt complexes prepared in this way were determined by X-ray crystallography. The results revealed that the cobalt ions in these complexes were tetrahedrally coordinated to two chloride anions and two nitrogen atoms from the pyridine and imidazole moieties of the ligand. The electrochemical properties of the ligands and their complexes were evaluated by cyclic voltammetry, and the results revealed that the first stage in the reduction of the Co(II) and Cu(II) complexes involved the reversible formation of the corresponding Co(I) and Cu(I) complexes, respectively. The cytotoxicity activities of the organic ligands and their complexes were evaluated against several cancer cell lines, including MCF-7, A549 and HEK293 cells. The copper complexes of the organic ligands bearing a phenyl or allyl moiety at their N(3) position together with a piperidine substituent at the 2-position of their imidazolone ring exhibited the greatest cytotoxicity of all of the compounds tested in the current study.     

Electron cooling experiments in CSR

The six species heavy ion beam was accumulated with the help of electron cooling in the main ring of Cooler Storage Ring of Heavy Ion Research Facility in Lanzhou (HIRFL-CSR). The ion beam accumulation dependence on the parameters of cooler was investigated experimentally. The 400 MeV/u ¹²C⁶⁺ and 200 MeV/u ¹²⁹Xe⁵⁴⁺ were stored and cooled in the experimental ring CSRe, and the cooling force was measured in different conditions.