190 research outputs found

    Effect of the Mechanism Transfer Function on the Positioning Law

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    Parametric synthesis of mechanical system consisting of actuator, transfer mechanism and control device is considered. Planar and spatial mechanisms with one degree of freedom can be included in the system. Mechanism structure and the type of the actuator are considered to be given preliminary.     Keywords: synthesis, mechanism, drive, contro

    (E)-2-(hydroxystyryl)-3-phenylquinazolin-4(3H)-ones: Synthesis, photochemical and luminescent properties

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    The new (E)-2-(hydroxyarilethenyl)-3-phenylquinazolin-4(3H)-ones with various substituents in phenyl fragment were synthesized. The effect of electron donor and acceptor substituents (±M) in quinazolinones on luminescence intensity and dual emission in 550-650-nm wavelength range was shown. The fact of the reversible photo/thermal E-Z isomerization for several substances was established. The (E)-2-(5-chloro-2-hydroxystyryl)-3-phenylquinazolin-4(3H)-one had shown the best combination of photochemical (E-Z isomerization) and photophysical properties. The (E)-2-(2-hydroxy-5-morpholinostyryl)-3-phenylquinazolin-4(3H)-one had revealed the best ESIPT-luminescence (Φrel = 5.3 %). © Arkat. All Rights Reserved.Russian Foundation for Basic Research, RFBR: 18-03-00112This work was supported by the Russian Foundation for Basic Research (grant 18-03-00112). Analytical studies were carried out using equipment of the Center for Joint Use SSpectroscopy and ?nalysis of Organic Compounds ? at the Postosvky Institute of Organic Synthesis of the Russian Academy of Sciences (Ural Branch)

    TIMELY DETECTION OF PULMONARY TUBERCULOSIS AND INFLUENCING FACTORS

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    This study presents analysis of the timely detection of pulmonary tuberculosis in 1334 patients who underwent treatment in the Regional TB Dispensary N1 in Krasnoyarsk city in 2010-2011. Late detection of tuberculosis was established in 60,2 %, and factors which are contributing to it were as following: the male, living in rural areas, social vulnerability, and. violation of the regulated terms of X-ray examination. The significance of late diagnosed patients to increase the reservoir of tuberculosis infection and spread of drug-resistant strains among the population was shown. It was determined that an increase in coverage of population by preventive X-ray examinations resulted in improvement of quality indicators only in 2,6 % of active detection of pulmonary tuberculosis in the form of growing proportion of the patients revealed during preventive examinations timely, as well as reducing proportion of fibro-cavernous pulmonary tuberculosis and. post-mortem diagnosis of tuberculosis among the newly diagnosed patients. During the active detection of TB among population with a focus of work on real, established during the research, its groups the conclusion about the need to use the obtained results was made

    Synthesis of 7-cycloalkylimino substituted 3-amino-6-fluoro-2-methyl-3H- quinazolin-4-ones

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    A versatile pathway for the synthesis of 7-cycloalkylimino substituted 3-amino-6-fluoro-2-methyl-3H-quinazolin-4-ones from 4,5-difluoroanthranylic acid has been advanced. Nucleophilic amination-defluorination reaction of the 6,7-difluoro derivative of 3-amino-2-methyl-3H-quinazolin-4-one has been established to occur at position 7, as shown by X-ray crystallographic analysis. © 2012 Elsevier B.V

    Vasotoxic Effects of Anticancer Therapy: a Review of Current Data

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    Cardiovascular and oncological diseases are the leading causes of adult death in the world. Despite proven efficacy, anticancer drugs can cause severe cardiovascular complications. Recently, data have appeared on the possible vasotoxic effects of chemotherapy drugs, which can manifest themselves as the progression of arterial hypertension and atherosclerosis, the development of myocardial ischemia and acute coronary syndrome, the formation of venous and arterial thrombosis. The key mechanism for the development of vasotoxicity is endothelial dysfunction, and anticancer drugs can also affect the processes of thrombosis. The review presents the results of 12 selected observational retro- and prospective studies involving cancer patients receiving presumably vasotoxic therapy. Data on the frequency of occurrence and possibilities for the prevention of vasotoxicity are presented

    MELT INCLUSIONS IN OLIVINE AS A SOURCE OF INFORMATION ON THE COMPOSITION AND EVOLUTION OF DEEP MELTS OF AILLIKITES (ULTRAMAFIC LAMPROPHYRES) OF THE ILBOKICHI UPLIFT, THE SW SIBERIAN PLATFORM

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    Aillikites are kimberlite-like rocks, important for understanding the composition and processes occurring in the mantle. Melt inclusions represent a reliable source of information. The paper provides the first results of studies (Raman, EDS) on primary and secondary melt inclusions in olivine from the Ilbokich uplift aillikites. The composition of primary inclusions is close to that of parent melt of aillikites. It was significantly enriched in CO2, H2O, phosphorus and titanium. Phlogopite, diopside, dolomite, calcite, apatite, Ti-containing phases (brookite, perovskite, Ti-magnetite) and lizardite were identified in these inclusions. The similarity of the composition and ratios of the daughter phases with the aillikite matrix indicates a slight change in the parent melt when it is rising to the surface. As to the secondary inclusions, there are wide variations in compositions and a smaller amount of silicates, as compared to the primary ones. The main daughter phases are carbonates, e.g. dolomite, calcite, magnesite and alkaline carbonates. In addition, phlogopite, clinopyroxene, apatite, halite, pyrrhotite and magnetite, graphite and CO2 were discovered. The variability of the compositions of the secondary inclusions might be due to the silicate-carbonate immiscibility that appeared during the rising of the aillikite melt at pressures <4 GPa

    Composition of oils of carbonate reservoirs in current and ancient water-oil contact zones

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    © 2015 Springer Science+Business Media New York. Differences in the composition of heavy oils from ancient and current water-oil contact (WOC) zones of productive strata of carbonate reservoirs of deposits of Bashkir and Turnei (Tatarstan) stages are discerned by applying a host of physicochemical methods, namely, elemental analysis, liquid-adsorption chromatography, gas chromatography, IR spectroscopy, and EPR spectroscopy. There is no direct connection of the composition of the hydrocarbons with the secondary changes of the reservoirs and their filtration-capacity parameters. Signs of seepage of light hydrocarbons are detected in the ancient WOC zones characterized by the presence of products of biochemical degradation of high-molecular-weight components of residual oil. This provides a basis for suggesting that these zones are not only fluid-supports but also migration channels for interstratal seepages of hydrocarbons during formation and development of oil reservoirs

    Верхнедевонские магматические комплексы юго-восточной Беларуси

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    For the first time, the authors determined lateral-temporal series of magmatic complexes of the Late Frasnian-Early Famennian Pripyat-Dnieper Magmatic Area according to the results of petrological and geochemical study of rocks of the Pripyat-Dnieper Magmatic Area (north-western part of the Pripyat-Dnieper-Donetsk Magmatic Province) in the southwest of the East European Platform using the principles of structural-material analysis and taking into account previous studies. The series consists of four complexes, formed during stages of magmatic activity, separated by time intervals: Zhlobin Complex (Rechitsa Time, the beginning of the Late Frasnian), Uvarovichi complex (Late Voronezh Time, the middle of the Late Frasnian), Pripyat Complex (Skolodin (Skolodin-Chernin?) Time, the end of the Late Frasnian) and Loev complex (Yelets (Yelets- Petrikov?) Time, Early Famennian). The rocks of the Zhlobin Complex belong to the alkaline-ultramafic (carbonatite-kimberlite-nephelinite) formation; Uvarovichi Complex - to the alkaline-mafic formation (basaltoids and phonolites); Pripyat Complex - to the alkaline-mafic-salic formation (trachyandesites); Loev Complex - to the alkaline-ultramafic (nepheline) formation.Впервые по результатам петролого-геохимического изучения пород Припятско-Днепровской области магматизма (северо-западная часть Припятско-Днепрово-Донецкой магматической провинции) на юго-западе Восточно-Европейской платформы с применением принципов структурно-вещественного анализа и с учетом ранее проведенных исследований авторами выделен латерально-временной ряд магматических комплексов позднефранско-раннефаменской Припятско-Днепровской области магматизма на юго-востоке Беларуси. Ряд состоит из четырех комплексов, сформированных в ходе этапов магматической активности, разделенных временными промежутками: жлобинского (речицкое время, начало позднего франа), уваровичского (поздневоронежское время, середина позднего франа), припятского (сколодинское (сколодинско-чернинское?) время, конец позднего франа) и лоевского (елецкое (елецко-петриковское?) время раннего фамена). Породы жлобинского комплекса принадлежат к щелочно-ультрамафитовой (карбонатит-кимберлит-нефелинитовой) формации; уваровичского комплекса - к щелочно-мафитовой формации (базальтоидов и фонолитов); припятского комплекса - к щелочно-мафическо-салической формации (трахиан-дезитов); лоевского комплекса - к щелочно-ультрамафитовой (нефелинитовой) формации

    Potential of primary drug prevention of cardiotoxicity in the context of anticancer therapy

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    Aim. To search early signs of cardiotoxicity in patients receiving anticancer therapy and evaluate the effectiveness of cardioprotection with an angiotensin-converting enzyme inhibitor, beta-blocker and myocardial cytoprotector.Material and methods. The study included 98 patients with high and very high risk of cardiotoxicity according to the Mayo Clinic scale (USA). Cancer patients with hypertension were offered cardioprotective treatment with a fixed-dose combination of perindopril and bisoprolol, and patients with very high risk and concomitant coronary artery disease additionally trimetazidine.The patients were divided into 2 following groups: the experimental group (n=50), where patients were prescribed cardioprotective therapy, and the control group (n=48), which consisted of patients who refused or had contraindications to cardioprotection. All patients underwent an examination, including the collection of complaints and anamnesis, physical examination, electrocardiography and echocardiography with an assessment of left ventricular (LV) global longitudinal strain before chemotherapy and 1, 3, 6, 9 and 12 months after initiation of anticancer therapy.Results. In patients of the control group, by the end of the follow-up, the left atrial volume index and LV end-diastolic volume index significantly increased. In the main group, these indicators did not change significantly. In the control group, by the final visit, the LV ejection fraction significantly decreased in comparison with the initial value and the value in the first group. After 6, 9 and 12 months, there was a significant decrease in the LV global longitudinal strain in the control group, while in the main group this indicator remained within the normal range. The mortality rate in the control group was significantly higher (15% vs 2% in the experimental group). In the experimental group, cardiotoxic complications occurred in 28%, while in the control group — in 78% of patients.Conclusion. The study demonstrated the significant importance of cardiac monitoring and primary drug prevention of cardiotoxicity of anticancer therapy. A sig nificant deterioration in LV systolic function was shown in patients with a high and very high risk of cardiotoxicity who did not receive cardioprotective therapy, while its high efficiency was demonstrated in patients of the experimental group

    Protein ruthenation and DNA alkylation: chlorambucil-functionalized RAPTA complexes and their anticancer activity

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    Chemotherapeutics for the treatment of tumorigenic conditions that feature novel modes of action are highly sought after to overcome the limitations of current chemotherapies. Herein, we report the conjugation of the alkylating agent chlorambucil to the RAPTA scaffold, a well-established pharmacophore. While chlorambucil is known to alkylate DNA, the RAPTA complexes are known to coordinate to amino acid side chains of proteins. Therefore, such a molecule combines DNA and protein targeting properties in a single molecule. Several chlorambucil-tethered RAPTA derivatives were prepared and tested for their cytotoxicity, stability in water and reactivity to protein and DNA substrates. The anticancer activity of the complexes is widely driven by the cytotoxicity of the chlorambucil moiety. However, especially in the cis-platin-resistant A2780R cells, the chlorambucil-functionalized RAPTA derivatives are in general more cytotoxic than chlorambucil and also a mixture of chlorambucil and the parent organoruthenium RAPTA compound. In a proof-of-principle experiment, the cross-linking of DNA and protein fragments by a chlorambucil-RAPTA derivative was observed
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