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It is well known that in modern micro- and nanoelectronics thin-film structures are actively used as a gate dielectric, passivating layers, membranes, etc. The research is devoted to the problem of crack formation in thin sublayers of silicon oxide during pulsed heating of interconnects on single-crystal silicon wafers. The purpose of the paper is to study the effect of surface sources of thermal shock on the cracks formation in films and aspects of crack formation in SO2 films have been studied in detail. Experimental verification of the estimates made was carried out on multilayer structures of a silicon substrate-silicon oxide sublayer-aluminum film (Si-SiO2-Al). As substrates, it was used phosphorus-doped silicon single-crystal wafers oriented in the (111) direction, with a resistivity in the range p = 0.1 Ω.сm. The authors studied the temperature fields in silicon wafers (Al-Si system) and silicon oxide wafers (Al-SiO2 system) heated by a surface metallization layer both for the case of a point heat source and for the case of a long rectangular metallization path (provided that the track length significantly exceeds its width). The calculation results showed that the temperature profile of the metallization path (width 75 μm) in the transverse direction is heterogeneous. It was also shown that, in contrast to SiO2 films, the level of appearing mechanical stresses in silicon is insufficient for the formation of cracks near the source of thermal shock. This is due to a higher tensile strength than that of oxide.

The work is devoted to the problem of crack formation in thin sublayers of silicon oxide during pulsed heating of interconnects on single-crystal silicon wafers. It was shown that the passage of current pulses with an amplitude of up to 8 × 1010 A/m2 and a duration of up to 500 μs leads to thermal destruction of the interconnects and contributes to the formation of microcracks in SiO2 films along the metallization path. The magnitude of the mechanical stresses arising in the structure during thermal shock is estimated. It is shown that in contrast to SiO2 films, the level of mechanical stresses in silicon is insufficient for cracking near the source of thermal shock. It was also found that the nature of cracking in a dielectric film depends on the quality of the deposition of the dielectric film and the metal film, as well as the state of the dielectric-metal interface.

A distributed temperature monitoring inside a cavity of ytterbium DFB and holmium fiber lasers has been demonstrated with a spatial resolution of 1 and 5 mm, respectively, for the first time to the best of our knowledge. For this, we use an optical backscatter reflectometer, which measures intracore temperature, and compare it with the data of an IR thermographic camera, which measures temperature from the surface of a fiber. In the case of holmium fiber laser pumped at a wavelength of 1125 nm with a power of 6 W, the maximum temperature variation along the ∼3-m active fiber reaches ∼60 °C. In the case of ytterbium DFB laser, we observe a strong inhomogeneity of the temperature along the DFB cavity, which leads to a significant decrease in the lasing efficiency. When pumped by a single-mode laser diode at a wavelength of 976 nm with a power of up to 526 mW, the maximum temperature difference reaches 37 °C for the 37-mm DBF cavity.

The work is devoted to processes during melting of thin aluminium film on silicon surface in pulse current mode. An experiment was conducted to study the dynamics during the onset of the liquid phase on a metal film. Besides, the process of formation droplet localization zones is considered. The experimental part revealed critical current values ​ during an electrical explosion of thin metal films near the thermal shock source. Using the oscillographic method, the temperature profile of the metallization track is calculated.

The composition of the intestinal microflora of rats with experimental antibiotic-associated dysbiosis and after its correction with a biological product based on lactic acid and propionic acid microorganisms was studied. The results obtained indicate the normalization of the number of microorganisms when using the suspension form of the drug and make it possible to recommend its use in clinical practice for the correction of intestinal microflora disorders in animals.

By cyclotrimerization of tert-butyl substituted pyrazine-2,3-dicarbonitrile in the presence of boron trichloride, two positional isomers ([Formula: see text] and [Formula: see text] symmetry) of the corresponding boron(III) tripyrazinosubporphyrazines were first obtained and efficiently separated by column chromatography. The new compounds were characterized by MALDI mass-spectrometry, UV-visible and 1H NMR spectroscopy. A Q-band in the electronic absorption spectra for both fractions was observed at [Formula: see text]530 nm, which is typical for tripyrazinosubporphyrazines. The fluorescence quantum yield for the regioisomer with lower symmetry ([Formula: see text] is 1.5 times higher than for the more symmerical [Formula: see text] species ([Formula: see text] = 0.37 and 0.28, respectively). Comparative spectrophotometric study of the basic properies reveals that hexaaza substitution in benzene rings of tert-butyl substituted subphthalocyanine decreases the basic properties of meso-nitrogen atoms.

Synthesis of new bis(seleno-imidazolone) derivatives bearing the alkyl and aryl moieties at the N(1) atom of the five-membered ring was developed. Cytotoxicity of the synthesized compounds against A549, VA-13, MCF-7, and HEK293T cell lines was evaluated.

New 3,5-disubstituted-1,2,4-thiadiazoles were synthesized and together with a series of their analogs obtained earlier were tested for cytotoxic activity to breast adenocarcinoma MCF-7 and lung carcinoma A 549 cells. The selectivity of cytotoxic action was determined in comparison to etiologically noncancerous breast epithelial cells MCF-10A and lung fibroblasts VA13. From five- to six-fold selectivity of cytotoxic action was revealed for 3,4-dichlorophenyl-{3-[2-(2-morpholin-4-ylethylamino)propyl]-[1,2,4]thiadiazol-5-yl}amine and (2-{5-[(4-diethylami-nobenzyl)pyridin-3-ylmethylamino]-[1,2,4]thiadiazol-3-yl}-1-methylvinyl)-(2,2,6,6-tetra-methylpiperidin-4-yl)amine in the pairs A 549/VA13 and MCF-7/MCF-10A, respectively. Some structure—property relationships for the compounds under study were discussed.

Electrophoretically homogeneous lectin with a specific activity of 100.0 U/mg protein was isolated and purified from the fungal mycelium of Fusarium solani 4. The molecular weight of the native lectin molecule (38 kDa) was determined. It was established that it consists of two identical subunits, with the molecular mass determined via PAGE-Na electrophoresis in the presence of DDS-Na equal to 19 kDa. The physicochemical properties and carbohydrate specificity of the lectin, as well as its in vitro effect on mammalian cancer cells, were studied. The results opened new prospects for the further study of lectin and its potential applications as a medical agent.

Abstract The reaction of lithium β-diketiminate [{2,6-Me2C6H3N=CMe}2CH]Li with benzophenone in toluene at 25°C affords the coordination complex [{2,6-Me2C6H3N=CMe}2CH]Li(Ph2C=O) (I). New keto-β-diketimine {2,6-Me2C6H3N=C(Me)}2CHC(tert-Bu)=O (II) is synthesized by the reaction of tert-Bu(C=O)Cl with [{2,6-Me2C6H3N=CMe}2CH]Li. The metallation of keto-β-diketimine II with n-butyllithium in THF at 0°C gives lithium keto-β-diketiminate {[{2,6-Me2C6H3N=C(Me)}2CС(tert-Bu)=O]Li(THF)}n (III). The exchange reaction of YCl3 with compound III (molar ratio 1 : 2, THF) affords the yttrium bis(keto-diketiminate) complex [{2,6-Me2C6H3N=C(Me)}2CС(tert-Bu)=O]2Y(μ2-Cl)2L-(THF)2 (IV). The molecular structures of complexes I, III, and IV are determined by X-ray diffraction analysis (CIF files CCDC nos. 2001131 (I), 2001132 (III), and 2001133 (IV)). Complex IV in the crystalline state exists as an ate complex with one LiCl molecule. Complexes I, III, and IV are catalysts of ring-opening polymerization of ε-caprolactone in toluene at 25°С.

On the basis of theoretical considerations and computer experiment, we suggest a new technique for separation of polymer molecules. The method is based on filling an array of nanochannels with macromolecules whereby the subsequent ejection time depends strongly on small differences in the end-to-end distances of elongated configurations inside the nanotubes. In contrast to conventional methods for chromatographic separation, the efficiency of the proposed method increases with growing molecular length of the chains. The method appears promising also for the separation of ring from linear polymer chains.

Synthesis, characterization (HRMS, NMR, EPR, UV-Vis spectroscopy, and electrochemistry) and in vitro cytotoxic investigation of a series of new ferrocene-containing derivatives, based on ω-ferrocene carboxylic acids and 2-alkylthioimidazolin-4-ones as well as their copper coordination compounds, have been reported. A series of ferrocene–imidazolone conjugates with different lengths and donor properties of the linker fragments have been synthesized; all the obtained compounds were studied in complexation reactions with copper(I) and copper(II) perchlorates. It is shown that the synthesised conjugates rapidly and efficiently convert coordinating copper ions into the Cu(+1) oxidation state, but a change in the length of the linker in ferrocene–imidazolone ligands fundamentally changes the ratio of products formed as a result of iron oxidation/copper reduction and complexation by various mechanisms. After comparing the data on the qualitative and quantitative composition of the reaction mixtures and the kinetic characteristics of the processes occurring in the mixtures of ferrocene–imidazolones with copper(II) perchlorate, a scheme of the ongoing reactions was proposed which may fully explain all the observed processes and products. It has been shown that the obtained bimetallic Cu/Fe coordination compounds are more toxic than cisplatin and induce apoptosis in micromolar concentrations on Hek-293 and MCF-7 cell lines.

In a recent research paper Dr. Suxing Jin et al. reported two multispecific PtIV complexes DNP and NP with non-steroidal anti-inflammatory drug naproxen (NPX) as the axial ligand(s). Herein, we clarify the mechanism of action of DNP, its therapeutic target and intracellular redox-status.

Background: The key issue in the development of novel antimicrobials is a rapid expansion of new bacterial strains resistant to current antibiotics. Indeed, World Health Organization has reported that bacteria commonly causing infections in hospitals and in the community, e.g. E. Coli, K. pneumoniae and S. aureus, have high resistance vs the last generations of cephalosporins, carbapenems and fluoroquinolones. During the past decades, only few successful efforts to develop and launch new antibacterial medications have been performed. This study aims to identify new class of antibacterial agents using novel high-throughput screening technique. Methods: We have designed library containing 125K compounds not similar in structure (Tanimoto coeff.< 0.7) to that published previously as antibiotics. The HTS platform based on double reporter system pDualrep2 was used to distinguish between molecules able to block translational machinery or induce SOS-response in a model E. coli system. MICs for most active chemicals in LB and M9 medium were determined using broth microdilution assay. Results: In an attempt to discover novel classes of antibacterials, we performed HTS of a large-scale small molecule library using our unique screening platform. This approach permitted us to quickly and robustly evaluate a lot of compounds as well as to determine the mechanism of action in the case of compounds being either translational machinery inhibitors or DNA-damaging agents/replication blockers. HTS has resulted in several new structural classes of molecules exhibiting an attractive antibacterial activity. Herein, we report as promising antibacterials. Two most active compounds from this series showed MIC value of 1.2 (5) and 1.8 μg/mL (6) and good selectivity index. Compound 6 caused RFP induction and low SOS response. In vitro luciferase assay has revealed that it is able to slightly inhibit protein biosynthesis. Compound 5 was tested on several archival strains and exhibited slight activity against gram-negative bacteria and outstanding activity against S. aureus. The key structural requirements for antibacterial potency were also explored. We found, that the unsubstituted carboxylic group is crucial for antibacterial activity as well as the presence of bulky hydrophobic substituents at phenyl fragment. Conclusion: The obtained results provide a solid background for further characterization of the 5'- (carbonylamino)-2,3'-bithiophene-4'-carboxylate derivatives discussed herein as new class of antibacterials and their optimization campaign.

Heating of a thin metal film on a semiconductor surface and the corresponding state of stress of the near-contact region are considered. The stress estimation procedure in case of the local pulsed heating of a metallized region on the semiconductor surface is described. The theoretical and experimental sizes of the deformed silicon substrate region are compared with each other. An experiment is carried out using rectangular current pulses. The stress–strain region, which depends on the electric pulse duration and amplitude, is estimated. Experimental evidence shows a strong heterogeneity of the metallization track after pulse passage.

A mechanical technique used to determine the surface residual stresses and four techniques used to harden samples are described. The diagrams of surface residual stresss in titanium and iron–chrome–nickel alloy samples before and after hardening are built based on experimental data. All titanium and iron–chrome–nickel alloy samples are found to exhibit compressive surface stresses after hardening. The compressive residual stresses in the external layers of the product increase its fatigue strength to ≈20%.

Ekaterina A Skomorokhova,1,2 Tatiana P Sankova,3 Iurii A Orlov,1 Andrew N Savelev,3 Daria N Magazenkova,3 Mikhail G Pliss,4,5 Alexey N Skvortsov,3 Ilya M Sosnin,1 Demid A Kirilenko,1,6 Ivan V Grishchuk,3 Elena I Sakhenberg,7 Elena V Polishchuk,1,8 Pavel N Brunkov,1,6 Alexey E Romanov,1,6 Ludmila V Puchkova,1– 3 Ekaterina Yu Ilyechova1,2 1International Research Center of Functional Materials and Devices of Optoelectronics, ITMO University, St. Petersburg, Russia; 2Department of Molecular Genetics, Research Institute of Experimental Medicine, St. Petersburg, Russia; 3Higher Engineering Physics School of the Institute of Physics, Nanotechnology and Telecommunications, Peter the Great St. Petersburg Polytechnic University, St. Petersburg, Russia; 4Department of Experimental Physiology and Pharmacology, Almazov National Medical Research Centre, St. Petersburg, Russia; 5Laboratory of Blood Circulation Biophysics, Pavlov First Saint Petersburg State Medical University, St. Petersburg, Russia; 6Center of Nanoheterostructures Physics, Ioffe Institute, Russian Academy of Sciences, St. Petersburg, Russia; 7Laboratory of Cell Protection Mechanisms, Institute of Cytology, Russian Academy of Sciences, St. Petersburg, Russia; 8Telethon Institute of Genetics and Medicine, Pozzuoli, Naples, ItalyCorrespondence: Ekaterina Yu Ilyechova Department of Molecular GeneticsResearch Institute of Experimental Medicine, Acad. Pavlov Street, 12, St. Petersburg 197376, RussiaTel +79217605274Fax +78122322307Email ilichevaey@itmo.ruPurpose: The ability of silver nanoparticles (AgNPs) of different sizes to influence copper metabolism in mice is assessed.Materials and Methods: AgNPs with diameters of 10, 20, and 75 nm were fabricated through a chemical reduction of silver nitrate and characterized by UV/Vis spectrometry, transmission and scanning electronic microscopy, and laser diffractometry. To test their bioactivity, Escherichia coli cells, cultured A549 cells, and C57Bl/6 mice were used. The antibacterial activity of AgNPs was determined by inhibition of colony-forming ability, and cytotoxicity was tested using the MTT test (viability, %). Ceruloplasmin (Cp, the major mammalian extracellular copper-containing protein) concentration and enzymatic activity were measured using gel-assay analyses and WB, respectively. In vitro binding of AgNPs with serum proteins was monitored with UV/Vis spectroscopy. Metal concentrations were measured using atomic absorption spectrometry.Results: The smallest AgNPs displayed the largest dose- and time-dependent antibacterial activity. All nanoparticles inhibited the metabolic activity of A549 cells in accordance with dose and time, but no correlation between cytotoxicity and nanoparticle size was found. Nanosilver was not uniformly distributed through the body of mice intraperitoneally treated with low AgNP concentrations. It was predominantly accumulated in liver. There, nanosilver was included in ceruloplasmin, and Ag-ceruloplasmin with low oxidase activity level was formed. Larger nanoparticles more effectively interfered with the copper metabolism of mice. Large AgNPs quickly induced a drop of blood serum oxidase activity to practically zero, but after cancellation of AgNP treatment, the activity was rapidly restored. A major fraction of the nanosilver was excreted in the bile with Cp. Nanosilver was bound by alpha-2-macroglobulin in vitro and in vivo, but silver did not substitute for the copper atoms of Cp in vitro.Conclusion: The data showed that even at low concentrations, AgNPs influence murine copper metabolism in size-dependent manner. This property negatively correlated with the antibacterial activity of AgNPs.Keywords: silver nanoparticles, copper status, ceruloplasmin, alpha-2-macroglobulin, bile, urine

Selective ligands of an urea-based prostate specific membrane antigen with a phenylalanine/tyrosine-based dipeptide linker and with a mingled chiral centers configuration and/or substituted aromatic fragments were prepared in seven steps by liquid- and in six steps by solid-phase synthesis. In vitro test for inhibiting the cleavage of N-acetylaspartylglutamate revealed the optimum linker containing l -phenylalanine in the structure on the N-terminus of a dipeptide chain.

Sub-Doppler resonances in caesium vapours are studied in a laser field produced by counterpropagating two-frequency light beams with mutually orthogonal linear polarisations. The beams are in resonance with optical transitions in the D1 line, the frequency difference of the field spectral components being equal to the hyperfine ground-state splitting in the Cs atom (∼9.2 GHz). It has already been shown that in this configuration, the hypercontrast effect can be observed for sub-Doppler resonances, which makes this configuration promising for the employment in new-generation miniature optical frequency standards. In the present work, two different two-frequency configurations are compared with each other and with the single-frequency configuration widely used in practice for observing saturated absorption resonances. The parameters of nonlinear resonances are measured at various temperatures of caesium vapours and at different optical field intensities. The results of the investigations performed make it possible to find an optimal two-frequency scheme for exciting nonlinear resonances and to estimate a potential of the scheme for its applications in quantum metrology.

A series of 73 ligands and 73 of their Cu+2 and Cu+1 copper complexes with different geometries, oxidation states of the metal, and redox activities were synthesized and characterized. The aim of the study was to establish the structure-activity relationship within a series of analogues with different substituents at the N(3) position, which govern the redox potentials of the Cu+2/Cu+1 redox couples, ROS generation ability, and intracellular accumulation. Possible cytotoxicity mechanisms, such as DNA damage, DNA intercalation, telomerase inhibition, and apoptosis induction, have been investigated. ROS formation in MCF-7 cells and three-dimensional (3D) spheroids was proven using the Pt-nanoelectrode. Drug accumulation and ROS formation at 40-60 μm spheroid depths were found to be the key factors for the drug efficacy in the 3D tumor model, governed by the Cu+2/Cu+1 redox potential. A nontoxic in vivo single-dose evaluation for two binuclear mixed-valence Cu+1/Cu+2 redox-active coordination compounds, 72k and 61k, was conducted.

The gas evolution dynamics has been studied during thermal oxidation of 0.15 and 0.2 mol L−1 solutions of N,N,N′,N’-tetra-n-octyldiglycolamide (TODGA) in Isopar M diluent with n-decanol depending on the concentration of nitric acid. The effect of irradiation of the system “TODGA in Isopar M with n-decanol” on the possibility of a thermal explosion has been determined. Weak exothermic effects were observed for non-irradiated and irradiated mixtures in the presence of 4 mol L−1 HNO3 at 170 °C. At a concentration of nitric acid in the aqueous phase of 8 mol L−1 or more, for non-irradiated and irradiated two-phase systems, the process passes into a thermal explosion mode.

Technological features of the growth of single crystal silicon carbide inevitably create condi-tions for the formation of crystal structure defects in them. A method is proposed for recognizing and analyzing a dislocation structure of single crystal silicon carbide based on the use of optical microscopy and a direct distribution neural network. The method was tested on homoepitaxial lay-ers of 4H-polytype silicon carbide. Software has been developed that allows building maps of the dislocation structure distribution over the surface of single crystal silicon carbide. The software was tested on digital images of the surface of silicon carbide epitaxial layers. The accuracy of recognition of dislocation structure was 95%. The dislocation mapping is used in the development of process technologies for reducing their density during the growth of single crystals.

The exchange reaction of anhydrous YbCl3 with [1,3-C6H4{NC(Ph)N(SiMe3)}2Li2(THF)2]2 (I) (4 : 3 molar ratio, THF) gave ansa-bis(amidinate) ytterbium complex [1,3-C6H4{NC(Ph)N(SiMe3)}2]3Yb2 (II) in which three bis(amidinate) ligands form µ-bridges between two Yb3+ ions. An X-ray diffraction study (CIF file CCDC no. 1964848) showed that the dimeric structure of II is formed upon simultaneous coordination of κ2-N,N-chelating moieties of three ligands to two ytterbium atoms.

This work describes the procedure for determining residual surface stresses using the mechanical method and four methods of hardening samples. The urgency of the problem stated in the article is due to the fact that surface tensile stresses arising in the manufacture of highly loaded parts can significantly reduce the mechanical, resource and fatigue characteristics of products. The aim of the study was to harden samples of titanium and iron-chromium-nickel alloys to improve their strength, fatigue and resource characteristics and determine residual stresses by layer-by-layer removal of the studied layers by electrochemical etching. The determination of surface residual stresses was carried out mechanically using a measuring and calculation complex during continuous etching of the metal from the test surface of the sample, which made it possible to measure the residual stresses at different depths and determine the energy of the surface stress state. Residual stresses were calculated from the deformation of the remaining part of the sample with a change in the depth of the studied layers. The hardening of the samples was carried out in four ways, namely: ultrasonic hardening; ultrasonic curing + Rosler (vibration processing); Rosler (vibration processing) + ultrasonic curing; Rosler (vibration processing) + ultrasonic hardening. The results of the study showed that the surface of the products is a weaker area than the inside. After quenching, surface compressive stresses arise for all samples of titanium and iron-chromium-nickel alloys. The preferred case of hardening is the second (ultrasonic hardening + centrifugal hardening). The presence of residual compressive stresses in the outer layers of the products increases their fatigue limit by ≈20%. The results of the work can be used to manufacture products with high mechanical, resource and fatigue characteristics.

Chronic intoxication with vinyl chloride and polyvinyl chloride in industrial conditions is an extremely relevant occupational condition caused by the high production of this material and severe long-term intoxication consequences. The nervous system is mostly affected, which results in the clinical pattern of chronic intoxication with vinyl chloride and polyvinyl chloride. However, in addition to the neurotoxic effect, vinyl chloride and its derivatives have immunotoxic, embryotoxic and carcinogenic effects. This necessitates timely and effective primary and secondary prevention and treatment of those engaged in vinyl chloride and polyvinyl chloride production.

A single-frequency all-fiber thulium doped laser with distributed feedback is presented. The fiber Bragg grating with a phase shift, which is the cavity of the laser, is written in a highly-doped 36-mm segment of the thulium-doped fiber. The highest power of the single-frequency generation on the wavelength of 1919 nm reaches up to 80 mW at the power of the pumping radiation of 1.1 W. The generation linewidth is equal to 70 kHz. Relative intensity noises of the optical radiation do not exceed the level of 70 dB/Hz with the maximum at the frequency of 1.2 MHz.

The article describes a clinical case of successful treatment of a patient with disseminated bilateral fibrous cavernous tuberculosis and extensive drug resistance, with preserved sensitivity to only one anti-tuberculosis drug; the fifth chemotherapy regimen and pleuropneumonectomy were used.

The increase in multi-drug resistant pathogenic bacteria is making our current arsenal of clinically used antibiotics obsolete, highlighting the urgent need for new lead compounds with distinct target binding sites to avoid cross-resistance. Here we report that the aromatic polyketide antibiotic tetracenomycin (TcmX) is a potent inhibitor of protein synthesis, and does not induce DNA damage as previously thought. Despite the structural similarity to the well-known translation inhibitor tetracycline, we show that TcmX does not interact with the small ribosomal subunit, but rather binds to the large subunit, within the polypeptide exit tunnel. This previously unappreciated binding site is located adjacent to the macrolide-binding site, where TcmX stacks on the noncanonical basepair formed by U1782 and U2586 of the 23S ribosomal RNA. Although the binding site is distinct from the macrolide antibiotics, our results indicate that like macrolides, TcmX allows translation of short oligopeptides before further translation is blocked.

Clathrate hydrates are nonstoichiometric crystalline inclusion compounds. Water acts as a "host lattice" and traps small guest molecules in stable cavities. One example, methane hydrates, are especially prevalent in situ at the seafloor. Although microorganism-produced proteins and polypeptides, including marine methylotroph porin proteins, can accelerate methane hydrate formation under conditions simulating their natural occurrence at the seafloor, the role that particular peptide sequences play in biocatalytic hydrate kinetics enhancement is unclear, especially the underlying molecular-level mechanisms. Here, we reveal the peptide-focused regulation of microorganisms' role in managing marine hydrates via an approximation mechanism of enzymatic catalysis accelerating hydrate formation. Aside from control of hydrate kinetics per se, we speculate that this peptide-centric mechanistic understanding could lead to a re-evaluation of the extent and geological importance of bioregulation of methane turnover in the biosphere.

Background: High-throughput screening (HTS) of large-compound libraries is a convenient and cost-effective tool for novel drug discovery. However, in many cases, HTS platforms are not well adapted to perform cell-based screening assay with simultaneous identification of the mechanism of action for active compounds. Methods: Previously, we have described a unique double-reporter system that can be used to reveal compounds having antibacterial activity. This construction is based on two genes of Katushka2S and RFP that encode proteins with different imaging signature. The upregulated expression of the first gene attributes directly to translation inhibition in prokaryotes while the high expression of the second one is unambiguously associated with DNA biosynthesis restriction (SOS-response). Results: In the current work, we have applied this system for the identification of novel smallmolecule compounds with antibacterial activity in HTS scale. Compounds were selected from the ChemDiv in-house collection (of total 47K molecules) following the maximum diversity in structure. Based on the obtained results, we have revealed a small series of tetrahydrocarbazole derivatives with antibacterial activity. The hit compound inhibited bacterial growth with a MIC value of 21 μg/ml and blocked DNA biosynthesis. No activity towards translation has been observed. In spite of a relatively moderate potency, as compared to the control sample (erythromycin, MIC=3 μg/ml), this molecule provides good selectivity index (SI>333, HEK239). Conclusion: Tetrahydrocarbazole derivatives can be properly regarded as an attractive starting point for further development and optimization.

Thermal stability of extraction systems containing N,N,N′,N ′-tetra-n-octyldiglycolamide (TODGA), di(N-ethyl-4-hexylanilide) 2,2′-bipyridine-6,6′-dicarboxylic acid (DYP-7), di(N-ethyl-4-fluoroanilide) of 2,6-pyridinecarboxylic acid Et(pFPh)DPA, di(N -ethyl-4-ethylanilide) of 2,2′-bipyridine-6,6′-dicarboxylic acid (DYP-9) under the conditions capable of causing emergencies, i.e., those unfavorable as regards the fire and explosion safety. It was found that irradiation with accelerated electrons of a TODGA–Isopar-М mixture in an n-alcohol affects the possibility of a thermal explosion and shown that the irradiation is accompanied by an intense evolution of gases. The possibility of passing from the oxidation of organic components of the system by nitric acid to the burning and explosion mode was evaluated. It was found that, with diamides used, the pressures of gaseous products of exothermic reactions are substantially lower than those with TODGA and TBP, which makes them promising extracting mixtures as regards the safety of the technological process.

Irradiation with accelerated electrons of an extraction mixture of 30% TBP in Isopar-M isoparaffin diluent on the lower temperature limit of flame propagation (Тl) has been studied. It was found that, under irradiation up to a dose of 2 MGy, the value of Тl of the extraction mixture may decrease to 45°С, which should be taken into account when organizing the technological process. It was shown that, when an irradiated extraction mixture is bubbled with air, the value of Тl nearly reaches the Тl of the starting solution.

A series of novel hydantoin-based dispiroindolinones as potential small-molecule inhibitors of p53–MDM2 protein–protein interaction were synthesized by two methods, using 2-arylidenehydantoins as starting materials. Some compounds demonstrate moderate cytotoxicity against cancer cell lines with IC50 in micromolar concentration range, which is comparable to nutlin-3. Two of the synthesized dispiroindolinones show p53-related activity in p53 reporter activation test.

A general model for predicting the IC50 value (concentration causing 50% inhibition of enzyme activity) was obtained. It combined data for 40 variants of neuraminidases of influenza virus A (7 serotypes) and B and three known neuraminidase inhibitors, oseltamivir, zanamivir, and peramivir and using data only on enthalpy contributions to the potential energy of the inhibitor/protein and substrate/protein complexes (MUNANA). The calculations have been adapted to the use software with support for graphics accelerators, which reduces the calculation time. The R2 values for predicting pIC50 values for test sets were in the range of 0.45−0.58, the average error was 0.7 (with the range of the pIC50 training set from 4.55 to 10.22).

In this paper, we examine the issues of the formation and propagation of melted zones during electric explosion of thin aluminum films on the oxidized silicon surface. A difference in the formation and propagation mechanisms of melted zones on the surface during the passage of a current pulse and after it was switched off is found. After the current pulse is switched off, the migration of melted zones is revealed to be determined by the temperature gradient near a local heat source. The temperature gradients are obtained from the dimensional dependence of the displacement rate, and the thermoelasticity coefficient that determines the dynamics of zone migration in the temperature gradient field is estimated.

This article deals with problems of pathogenesis, clinical symptomatology, approaches to detection and treatment of acute and chronic chlorine intoxication.

The amplitude dependence of the internal friction (ADIF) of zirconium and Zr–8.1% Nb and Zr–20.2% Nb alloys has been investigated after different heat-treatment regimes. ADIF components caused by the processes of enhanced dissipation of energy at twin boundaries and at the boundaries of ω–β phases under mechanical vibrations have been revealed. The effect of twins, athermal, and isothermal ω phases, and the dislocation structure on the ADIF has been analyzed. A comparative analysis of the studied materials and their states in damping ability has been performed.

The adherence of Proteus mirabilis to the surface of urinary catheters leads to colonization and eventual blockage of the catheter lumen by unique crystalline biofilms produced by these opportunistic pathogens, making P. mirabilis one of the leading causes of catheter-associated urinary tract infections. The Proteus biofilms reduce efficiency of antibiotic-based treatment, which in turn increases the risk of antibiotic resistance development. Bacteriophages and their enzymes have recently become investigated as alternative treatment options. In this study, a novel Proteus bacteriophage (vB_PmiS_PM-CJR) was isolated from an environmental sample and fully characterized. The phage displayed depolymerase activity and the subsequent genome analysis revealed the presence of a pectate lyase domain in its tail spike protein. The protein was heterologously expressed and purified, the ability of the purified tail spike to degrade Proteus biofilms was tested. We showed that the application of the tail spike protein was able to reduce the adherence of bacterial biofilm to plastic pegs in a MBEC (minimum biofilm eradication concentration) assay and improve the survival of Galleria mellonella larvae infected with Proteus mirabilis. Our study is the first to successfully isolate and characterize a biofilm depolymerase from a Proteus phage, demonstrating the potential of this group of enzymes in treatment of Proteus infections.