708 research outputs found

    Dielectric properties of marsh vegetation

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    The present work is devoted to the measurement of the dielectric properties of mosses and lichens in the frequency range from 500 MHz to 18 GHz. Subjects of this research were three species of march vegetation – moss (Dicranum polysetum Michx), groundcedar (Diphasiastrum complanatum (L.) Holub) and lichen (Cladonia stellaris). Samples of vegetation were collected in Tomsk region, Western Siberia, Russia. Complex dielectric permittivity was measured in coaxial section by Agilent Technologies vector network analyzer E8363B. Green samples was measured for some moisture contents from 100% to 3–5 % during a natural drying. The measurements were performed at room temperature, which remained within 21 Γ· 23 Β° C. The frequency dependence of the dielectric constant for the three species of marsh vegetation differ markedly. Different parts of the complex permittivity dependency on moisture were fitted by line for all frequency points. Two break point were observed corresponding to the transition of water in the vegetation in various phase states. The complex permittivity spectra of water in the vegetation allow determining the most likely corresponding dielectric model of water in the vegetation by the method of hypothesis testing. It is the Debye’s model. Parameters of Debye’s model were obtained by numerical methods for all of three states of water. This enables to calculate the dielectric constant of water at any frequency range from 500 MHz to 18 GHz and to find the parameters of the dielectric model of the vegetation

    Outpatient management of patients with peripheral artery disease by cardiologists or surgeons: influence on the prognosis and prevalence of surgical interventions

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    Highlights. The study shows for the first time that during the three-year follow-up of patients with diseases of the arteries of the lower extremities in the observation groups of a general surgeon and a cardiologist, adverse events (myocardial infarction, stroke, amputation, disability) and deaths occurred more often in a surgeon than a cardiologist. The study proves the correctness and real benefit of such an approach with the involvement of a cardiologist to the outpatient stage of management of a complex cohort of patients with atherosclerosis of the vessels of the lower extremities.Aim. To study the effect the outpatient observation of patients with peripheral arteries disease (PAD) by cardiologists and surgeons has on timing and prevalence of reconstructive surgery and the prognosis of patients. Methods We analyzed the data on 585 PAD patients who underwent outpatient observation from 2010 to 2017, dividing them into 2 groups. The first group (131 patients) managed by an surgeon; the second (454 patients) managed by a cardiologist. Since the groups were not comparable in terms of the initial parameters, the comparability of patients in the groups (observation by a surgeon or by a cardiologist) was achieved using pseudorandomization. The follow-up period was three years; we assessed the incidence of deaths, adverse events, and the prevalence of reconstructive operations.Results. During a three-year follow-up the 1st group, compared with the 2nd, had more deaths in general (p<0.001), death from cardiac causes (p = 0.045), from stroke (p><0.001), as well as the total number of adverse events (p><0.001) and disability (p = 0.065). Indications for reconstructive surgery on the lower extremities arteries (LEA), and operations frequency were comparatible in groups. Amputation history, taking diuretics, presence of rhythm disturbances, and management by a surgeon increased the risk of adverse outcomes. Management by a cardiologist, reconstructive LEA surgeries, female sex improved the prognosis of patients. Conclusion Observation of PAD patients by a cardiologist contributes to a higher frequency of optimal drug therapy by patients and can reduce the number of adverse events in patients and improve their survival without affecting the timing and frequency of reconstructive LEA surgeries. Keywords Peripheral atherosclerosis β€’ Outpatient follow-up β€’ Optimal drug therapy β€’ Reconstructive surgery>Λ‚ 0.001), death from cardiac causes (p = 0.045), from stroke (pΛ‚ 0.001), as well as the total number of adverse events (pΛ‚ 0.001) and disability (p = 0.065). Indications for reconstructive surgery on the lower extremities arteries (LEA), and operations frequency were comparatible in groups. Amputation history, taking diuretics, presence of rhythm disturbances, and management by a surgeon increased the risk of adverse outcomes. Management by a cardiologist, reconstructive LEA surgeries, female sex improved the prognosis of patients.Conclusion. Observation of PAD patients by a cardiologist contributes to a higher frequency of optimal drug therapy by patients and can reduce the number of adverse events in patients and improve their survival without affecting the timing and frequency of reconstructive LEA surgeries.Highlights. The study shows for the first time that during the three-year follow-up of patients with diseases of the arteries of the lower extremities in the observation groups of a general surgeon and a cardiologist, adverse events (myocardial infarction, stroke, amputation, disability) and deaths occurred more often in a surgeon than a cardiologist. The study proves the correctness and real benefit of such an approach with the involvement of a cardiologist to the outpatient stage of management of a complex cohort of patients with atherosclerosis of the vessels of the lower extremities.Aim. To study the effect the outpatient observation of patients with peripheral arteries disease (PAD) by cardiologists and surgeons has on timing and prevalence of reconstructive surgery and the prognosis of patients. Methods We analyzed the data on 585 PAD patients who underwent outpatient observation from 2010 to 2017, dividing them into 2 groups. The first group (131 patients) managed by an surgeon; the second (454 patients) managed by a cardiologist. Since the groups were not comparable in terms of the initial parameters, the comparability of patients in the groups (observation by a surgeon or by a cardiologist) was achieved using pseudorandomization. The follow-up period was three years; we assessed the incidence of deaths, adverse events, and the prevalence of reconstructive operations.Results. During a three-year follow-up the 1st group, compared with the 2nd, had more deaths in general (p<0.001), death from cardiac causes (p = 0.045), from stroke (p><0.001), as well as the total number of adverse events (p><0.001) and disability (p = 0.065). Indications for reconstructive surgery on the lower extremities arteries (LEA), and operations frequency were comparatible in groups. Amputation history, taking diuretics, presence of rhythm disturbances, and management by a surgeon increased the risk of adverse outcomes. Management by a cardiologist, reconstructive LEA surgeries, female sex improved the prognosis of patients. Conclusion Observation of PAD patients by a cardiologist contributes to a higher frequency of optimal drug therapy by patients and can reduce the number of adverse events in patients and improve their survival without affecting the timing and frequency of reconstructive LEA surgeries. Keywords Peripheral atherosclerosis β€’ Outpatient follow-up β€’ Optimal drug therapy β€’ Reconstructive surgery>Λ‚ 0.001), death from cardiac causes (p = 0.045), from stroke (pΛ‚ 0.001), as well as the total number of adverse events (pΛ‚ 0.001) and disability (p = 0.065). Indications for reconstructive surgery on the lower extremities arteries (LEA), and operations frequency were comparatible in groups. Amputation history, taking diuretics, presence of rhythm disturbances, and management by a surgeon increased the risk of adverse outcomes. Management by a cardiologist, reconstructive LEA surgeries, female sex improved the prognosis of patients.Conclusion. Observation of PAD patients by a cardiologist contributes to a higher frequency of optimal drug therapy by patients and can reduce the number of adverse events in patients and improve their survival without affecting the timing and frequency of reconstructive LEA surgeries

    Master Education and Academic Career Track in Russia

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    The master’s degree is an obligatory stage for those who are planning to enter PhD. That is why it should have a clear academic track. Embedding the master’s degree in the academic track allows universities to sum up their efforts to support young scientists. There is an urgent need to support scientific centers in Russian universities. When the universities are competing for academic leadership, academic tracks become the ground for the development strategies.Previous researches showed that most students were ready to choose an academic track when they were master’s students. Thus, the academic track starts long before entering the doctoral programs. The study results reveal that master’s students do not have an opportunity to build an individual academic track within β€œhybrid” master’s programs. The Russian master’s degree programs shortly involve young researchers in projects, and this applies to all types of universities, including the research ones. The structure and ways of involving students in science do not differ in undergraduate and postgraduate programs. Master’s students who choose academic track do it without changing the major program. However, this trend doesn’t cover all the students. Master’s students use academic tracks to upgrade their professional skills for the further career but not at university or scientific institution

    Ehancement of security culture using a predictive model to prevent sabotage and theft at radiological facilities

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    Π‘Π ΠΠ’ΠΠ˜Π’Π•Π›Π¬ΠΠΠ― ΠžΠ¦Π•ΠΠšΠ ΠŸΠžΠšΠΠ—ΠΠ’Π•Π›Π•Π™ ΠŸΠžΠ‘Π’Π˜ΠΠ€ΠΠ ΠšΠ’ΠΠžΠ“Πž Π Π•ΠœΠžΠ”Π•Π›Π˜Π ΠžΠ’ΠΠΠ˜Π― Π›Π•Π’ΠžΠ“Πž Π–Π•Π›Π£Π”ΠžΠ§ΠšΠ Π’ Π—ΠΠ’Π˜Π‘Π˜ΠœΠžΠ‘Π’Π˜ ОВ ВАКВИКИ Π›Π•Π§Π•ΠΠ˜Π― ΠžΠ‘Π’Π ΠžΠ“Πž ИНЀАРКВА ΠœΠ˜ΠžΠšΠΠ Π”Π

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    Comparative assessment of the indices of post-infarction remodelling of the left ventricle was carried out in the patients with myocardium reperfusion (thrombolytic therapy) and without reperfusion. ECG was performed for all patients on admission to the hospital and then 3 and 6 months later. The results obtained demonstrated that after the acute period of myocardial infarction there was no difference between the parameters under control. At the same time the results of dynamic monitoring confirmed that later on the patients felt some peculiarities during the left ventricle remodelling process. Three months later there was an increase of the left ventricle sphericity index during the systoly in the patients of group II. Six months later the patients of group II showed significant difference in five indices of remodelling versus the patients on thrombolitic therapy.ВсСм Π±ΠΎΠ»ΡŒΠ½Ρ‹ΠΌ ΠΏΡ€ΠΎΠ²ΠΎΠ΄ΠΈΠ»ΠΎΡΡŒ эхокардиографичСскоС исслСдованиС ΠΏΡ€ΠΈ поступлСнии Π² стационар, Π° Ρ‚Π°ΠΊΠΆΠ΅ Ρ‡Π΅Ρ€Π΅Π· 3 ΠΈ 6 мСсяцСв. ΠŸΠΎΠ»ΡƒΡ‡Π΅Π½Π½Ρ‹Π΅ Π΄Π°Π½Π½Ρ‹Π΅ ΠΏΠΎΠΊΠ°Π·Π°Π»ΠΈ, Ρ‡Ρ‚ΠΎ ΠΏΠΎ ΠΎΠΊΠΎΠ½Ρ‡Π°Π½ΠΈΠΈ острого ΠΏΠ΅Ρ€ΠΈΠΎΠ΄Π° ΠΈΠ½Ρ„Π°Ρ€ΠΊΡ‚Π° ΠΌΠΈΠΎΠΊΠ°Ρ€Π΄Π° Π² Ρ€Π΅ΠΌΠΎΠ΄Π΅Π»ΠΈΡ€ΠΎΠ²Π°Π½ΠΈΠΈ Π›Π– практичСски Π½Π΅ наблюдалось сущСствСнных Ρ€Π°Π·Π»ΠΈΡ‡ΠΈΠΉ ΠΏΠΎ всСм ΠΊΠΎΠ½Ρ‚Ρ€ΠΎΠ»ΠΈΡ€ΡƒΠ΅ΠΌΡ‹ΠΌ ΠΏΠ°Ρ€Π°ΠΌΠ΅Ρ‚Ρ€Π°ΠΌ. Π’ Ρ‚ΠΎ ΠΆΠ΅ врСмя Ρ€Π΅Π·ΡƒΠ»ΡŒΡ‚Π°Ρ‚Ρ‹ динамичСского наблюдСния ΡΠ²ΠΈΠ΄Π΅Ρ‚Π΅Π»ΡŒΡΡ‚Π²ΠΎΠ²Π°Π»ΠΈ, Ρ‡Ρ‚ΠΎ Π² дальнСйшСм ΠΏΡ€ΠΎΡΠ²ΠΈΠ»ΠΈΡΡŒ сущСствСнныС особСнности Π² Ρ‚Π΅Ρ‡Π΅Π½ΠΈΠΈ процСсса рСмодСлирования Π›Π–. Π§Π΅Ρ€Π΅Π· Ρ‚Ρ€ΠΈ мСсяца ΠΎΡ‚ΠΌΠ΅Ρ‡Π°Π»ΠΎΡΡŒ нарастаниС индСкса сфСричности Π›Π– Π² систолу Ρƒ Π±ΠΎΠ»ΡŒΠ½Ρ‹Ρ… II Π³Ρ€ΡƒΠΏΠΏΡ‹. Π§Π΅Ρ€Π΅Π· ΡˆΠ΅ΡΡ‚ΡŒ мСсяцСв Π² Π³Ρ€ΡƒΠΏΠΏΠ΅ консСрвативного лСчСния наблюдалось достовСрноС Ρ€Π°Π·Π»ΠΈΡ‡ΠΈΠ΅ ΡƒΠΆΠ΅ ΠΏΠΎ пяти показатСлям рСмодСлирования Π›Π– (КБР, КБО, УО, ИББ, МББ), Π² ΠΎΡ‚Π»ΠΈΡ‡ΠΈΠ΅ ΠΎΡ‚ Π³Ρ€ΡƒΠΏΠΏΡ‹ Π±ΠΎΠ»ΡŒΠ½Ρ‹Ρ…, ΠΏΠΎΠ»ΡƒΡ‡Π°Π²ΡˆΠΈΡ… Ρ‚Ρ€ΠΎΠΌΠ±ΠΎΠ»ΠΈΡ‚ΠΈΡ‡Π΅ΡΠΊΡƒΡŽ Ρ‚Π΅Ρ€Π°ΠΏΠΈΡŽ

    Neuromuscular disorders in chronic alcohol intoxication

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    The paper reviews the present-day Russian and foreign literature on neuromuscular disorders in chronic alcohol intoxication. The most commonΒ manifestations of alcohol disease include alcoholic polyneuropathy (PNP) and alcohol-induced skeletal muscle injury. The clinical polymorphismΒ of alcoholic PNP is discussed. The paper considers a chronic sensory automatic form due to the direct toxic effects of ethanol and itsΒ metabolites during long-term alcohol intoxication, as well as acute/subacute sensorimotor neuropathy, the basis for the pathogenesis of whichΒ is B group vitamins, predominantly thiamine, deficiency that develops in the presence of drinking bouts concurrent with malnutrition and/orΒ alcohol-related gastrointestinal tract diseases. In addition to nonuse of alcohol and a properly balanced diet, antioxidant therapy with alphalipoicΒ acid and neurotropic B group vitamins is considered to be pathogenetic therapy for neuropathy. The most common and least studied clinicalform of alcohol-induced musculoskeletal injury is chronic alcoholic myopathy (AM), the diagnostic standard for which is morphometricand immunohistochemical examination of a muscle biopsy specimen. The morphological base for this form of myopathy is predominantly typeΒ 2 muscle fiber atrophy caused by impaired protein synthesis and a decreased regenerative potential of muscle fiber. The efficacy of antioxidantsΒ and leucine-containing amino acid mixtures in the treatment of chronic AM is discussed

    Clinical and psychological correlations with type D personality in patients with chronic coronary syndrome

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    Recently, it has become common to identify type D personality, which is predisposed to the development of psychological distress. Negative behavioral characteristics of individuals with type D personality contribute not only to the development of cardiovascular diseases, but also to Β other comorbid pathologies that can influence the progression and prognosis of coronary heart disease. The aim of the study. To identify clinical and psychological correlations with type D personality in patients with chronic coronary syndrome. Methods. The study included 113 patients (68 men and 45 women; median age – 64 years) admitted for planned percutaneous coronary intervention at the Research Institute for Complex Issues of Cardiovascular Diseases (Kemerovo, Russian Federation). Based on the results of the DS-14 test, patients were divided into two groups: patients with type D personality (n = 40) and patients without this type (n = 73). Results. In patients with chronic coronary syndrome with type D personality, compared with patients without this type, concomitant diabetes mellitus (35 % and 15 %, respectively; p = 0.018), signs of diastolic dysfunction of left (Π•/С’ ratio 7.1 [6.48; 8.0] and 5.0 [4.55; 5.74], respectively; p = 0.0038) and right (Et/At ratio – 0.8 [0.66; 1.35] and 1.38 [1.28; 1.63], respectively; p = 0.014) ventricles were more often diagnosed. Correlation analysis revealed associations of diabetes mellitus with type D personality (r = 0.243; p = 0.011), severity of negative excitability (r = 0.253; p = 0.008) and social suppression (r = 0.224; p = 0.020), as well as association of ankle-brachial index (ABI) with the severity of negative excitability (r = 0.393; p = 0.004) and social suppression (r = 0.414; p = 0.002). Conclusion. In patients having chronic coronary syndrome with type D personality, concomitant diabetes mellitus, as well as left and right ventricular filling disorders are Β more often detected. Correlation analysis revealed associations of diabetes mellitus with type Β D personality and its subscales; the ABI level was associated with subscales of type D personality, but not with the level of anxiety and depression

    The Institutional Support of Master Studies in Russia: Non-Commercial Actors and the Effects of their Influence

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    Π’ Π΄Π°Π½Π½ΠΎΠΉ ΠΈΡΡΠ»Π΅Π΄ΠΎΠ²Π°Ρ‚Π΅Π»ΡŒΡΠΊΠΎΠΉ ΡΡ‚Π°Ρ‚ΡŒΠ΅ освСщСны Ρ€Π΅Π·ΡƒΠ»ΡŒΡ‚Π°Ρ‚Ρ‹ изучСния ΠΏΡ€Π°ΠΊΡ‚ΠΈΠΊ ΠΈΠ½ΡΡ‚ΠΈΡ‚ΡƒΡ†ΠΈΠΎΠ½Π°Π»ΡŒΠ½ΠΎΠΉ ΠΏΠΎΠ΄Π΄Π΅Ρ€ΠΆΠΊΠΈ ΠΏΡ€Π΅ΠΏΠΎΠ΄Π°Π²Π°Ρ‚Π΅Π»Π΅ΠΉ магистратуры нСгосударствСнным ΡΡƒΠ±ΡŠΠ΅ΠΊΡ‚ΠΎΠΌ. ΠžΡ‚ΡΠ»Π΅ΠΆΠ΅Π½Ρ‹ Ρ‚Ρ€Π΅ΠΊΠΈ внСдрСния ΠΈ ΠΆΠΈΠ·Π½Π΅Π½Π½Ρ‹ΠΉ Ρ†ΠΈΠΊΠ» ΠΎΠ±Ρ€Π°Π·ΠΎΠ²Π°Ρ‚Π΅Π»ΡŒΠ½ΠΎΠ³ΠΎ ΠΏΡ€ΠΎΠ΄ΡƒΠΊΡ‚Π° Π² магистратурС, созданного ΠΏΡ€ΠΈ ΠΏΠΎΠ΄Π΄Π΅Ρ€ΠΆΠΊΠ΅ Π‘Π»Π°Π³ΠΎΡ‚Π²ΠΎΡ€ΠΈΡ‚Π΅Π»ΡŒΠ½ΠΎΠ³ΠΎ Ρ„ΠΎΠ½Π΄Π° Π’Π»Π°Π΄ΠΈΠΌΠΈΡ€Π° ΠŸΠΎΡ‚Π°Π½ΠΈΠ½Π° – СдинствСнного нСкоммСрчСского Ρ„ΠΎΠ½Π΄Π°, Ρ€Π΅Π°Π»ΠΈΠ·ΡƒΡŽΡ‰Π΅Π³ΠΎ ΠΏΡ€ΠΎΠ³Ρ€Π°ΠΌΠΌΡƒ ΠΏΠΎΠ΄Π΄Π΅Ρ€ΠΆΠΊΠΈ студСнтов ΠΈ ΠΏΡ€Π΅ΠΏΠΎΠ΄Π°Π²Π°Ρ‚Π΅Π»Π΅ΠΉ магистратуры. УстановлСно, Ρ‡Ρ‚ΠΎ Π² систСмС Ρ†Π΅Π½Ρ‚Ρ€Π°Π»ΠΈΠ·ΠΎΠ²Π°Π½Π½ΠΎΠ³ΠΎ государствСнного рСгулирования нСгосударствСнная ΠΏΠΎΠ΄Π΄Π΅Ρ€ΠΆΠΊΠ° ΠΏΡ€Π΅ΠΏΠΎΠ΄Π°Π²Π°Ρ‚Π΅Π»Π΅ΠΉ магистратуры вносит Π·Π½Π°Ρ‡ΠΈΠΌΡ‹ΠΉ Π²ΠΊΠ»Π°Π΄ Π² ΠΈΠ·ΠΌΠ΅Π½Π΅Π½ΠΈΠ΅ Π΅Π΅ Ρ€ΠΎΠ»ΠΈ Π² Π²Ρ‹ΡΡˆΠ΅ΠΌ ΠΎΠ±Ρ€Π°Π·ΠΎΠ²Π°Π½ΠΈΠΈ. ΠžΠ±ΠΎΠ·Π½Π°Ρ‡Π΅Π½Ρ‹ ΠΊΠΎΠ½Ρ‚ΡƒΡ€Ρ‹ долгосрочных эффСктов этой ΠΏΠΎΠ΄Π΄Π΅Ρ€ΠΆΠΊΠΈ, связанныС с Ρ„ΠΎΡ€ΠΌΠΈΡ€ΠΎΠ²Π°Π½ΠΈΠ΅ΠΌ срСды для развития Ρ‚Π°Π»Π°Π½Ρ‚ΠΎΠ², ΠΏΠΎΠ²Ρ‹ΡˆΠ΅Π½ΠΈΠ΅ΠΌ ΠΎΠ±Ρ€Π°Π·ΠΎΠ²Π°Ρ‚Π΅Π»ΡŒΠ½Ρ‹Ρ… Ρ€Π΅Π·ΡƒΠ»ΡŒΡ‚Π°Ρ‚ΠΎΠ² студСнтов, ΠΊΠ²Π°Π»ΠΈΡ„ΠΈΠΊΠ°Ρ†ΠΈΠΈ ΠΏΡ€Π΅ΠΏΠΎΠ΄Π°Π²Π°Ρ‚Π΅Π»Π΅ΠΉ, Π° Ρ‚Π°ΠΊΠΆΠ΅ ΠΈΠ½Ρ‚Π΅Π³Ρ€Π°Ρ†ΠΈΠΈ магистСрских ΠΏΡ€ΠΎΠ³Ρ€Π°ΠΌΠΌ Π² стратСгичСскиС Ρ†Π΅Π»ΠΈ развития унивСрситСта ΠΈ Ρ€Π΅Π³ΠΈΠΎΠ½Π°. Π‘Ρ‚Π°Ρ‚ΡŒΡ Π±ΡƒΠ΄Π΅Ρ‚ ΠΏΠΎΠ»Π΅Π·Π½Π° исслСдоватСлям Π²Ρ‹ΡΡˆΠ΅Π³ΠΎ образования, прСподаватСлям ΠΈ руководитСлям магистСрских ΠΏΡ€ΠΎΠ³Ρ€Π°ΠΌΠΌ, администраторам Π²ΡƒΠ·ΠΎΠ², Π»ΠΈΡ†Π°ΠΌ, ΠΏΡ€ΠΈΠ½ΠΈΠΌΠ°ΡŽΡ‰ΠΈΠΌ Ρ€Π΅ΡˆΠ΅Π½ΠΈΡ Π² области трансформации Π²Ρ‹ΡΡˆΠ΅Π³ΠΎ образования Π² России.This paper presents the results of studying non-state actors’ institutional support for masters’ teachers. The authors analyze the tracks of the introduction and a Β«life cycleΒ» of the master’s educational product created with the support of the Vladimir Potanin Foundation – the only non-commercial organization in Russia which supports students and professors at the master’s level. The study shows that the support for masters’ teachers makes a significant contribution to changing the role of this degree in higher education. There are outlined the long-term effects of supporting masters’ teachers, which are supposed to create an environment for developing talents, improving the educational results of master students, teachers’ advanced training, and integrating master programs into university’s and region’s strategic goals of development. For higher education researchers, for teachers and managers of master programs, for university administrators, and for higher education transformation decision makers in Russia

    АминированиС эпоксидов ΠΊΠ°ΠΊ ΡƒΠ΄ΠΎΠ±Π½Ρ‹ΠΉ способ синтСза Π»ΠΈΠΏΠΎΡ„ΠΈΠ»ΡŒΠ½Ρ‹Ρ… ΠΏΠΎΠ»ΠΈΠ°ΠΌΠΈΠ½ΠΎΠ²

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    Objectives. Alkylated derivatives of polyamines are able to block the growth of cancer cells due to their embedding into the polyamine biosynthesis mechanisms. The study aimed to synthesize lipophilic derivatives of norspermine or triethylenetetramine based on the formation of a C–N bond during the opening of the oxirane ring by primary amines to expand a number of synthetic polyamine derivatives with antitumor activity.Methods. The starting compoundsβ€”glycidol alcoholate or epichlorohydrinβ€”were reacted with hexadecyl bromide or sodium hexadecanolate to give glycidyl hexadecyl ether. The key reaction for the preparation of lipophilic polyamines was the amination of lipophilic epoxides with polyamines in the presence of calcium triflate. Acylation of the hydroxyl group formed during the opening of oxirane was carried out by the action of 4-dimethylaminopyridine and acetic anhydride. The introduction of an alkyl substituent in the presence of sodium hydride led to intramolecular cyclization with the formation of an oxoazolidine cycle. The regioselectivity of the oxirane ring opening reaction at the C(1) position of glycerol was confirmed by two-dimensional heteronuclear {1H,13C} nuclear magnetic resonance spectroscopy.Results. An approach to the synthesis of novel lipophilic polyamines based on the catalytic amination of epoxides was developed and tested. Compounds based on norspermine and triethylentetramine containing a hydroxyl group at the C(2) atom of the glycerin backbone were obtained. For norspermine derivatives, the hydroxyl group was modified: an acetyl substituent was introduced and a derivative containing an oxoazolidine cycle was obtained.Conclusions. The obtained lipophilic polyamines can be considered as potential antitumor agents, for which cytotoxicity against various cancer cells will be evaluated in the future.Π¦Π΅Π»ΠΈ. АлкилированныС ΠΏΡ€ΠΎΠΈΠ·Π²ΠΎΠ΄Π½Ρ‹Π΅ ΠΏΠΎΠ»ΠΈΠ°ΠΌΠΈΠ½ΠΎΠ² способны Π±Π»ΠΎΠΊΠΈΡ€ΠΎΠ²Π°Ρ‚ΡŒ рост Ρ€Π°ΠΊΠΎΠ²Ρ‹Ρ… ΠΊΠ»Π΅Ρ‚ΠΎΠΊ Π·Π° счСт встраивания Π² ΠΌΠ΅Ρ…Π°Π½ΠΈΠ·ΠΌΡ‹ биосинтСза ΠΏΠΎΠ»ΠΈΠ°ΠΌΠΈΠ½ΠΎΠ². ЦСль исслСдования – ΡΠΈΠ½Ρ‚Π΅Π·ΠΈΡ€ΠΎΠ²Π°Ρ‚ΡŒ Π½ΠΎΠ²Ρ‹Π΅ Π»ΠΈΠΏΠΎΡ„ΠΈΠ»ΡŒΠ½Ρ‹Π΅ ΠΏΡ€ΠΎΠΈΠ·Π²ΠΎΠ΄Π½Ρ‹Π΅ норспСрмина ΠΈΠ»ΠΈ триэтилСнтСтрамина, основанныС Π½Π° Ρ„ΠΎΡ€ΠΌΠΈΡ€ΠΎΠ²Π°Π½ΠΈΠΈ связи C–N ΠΏΡ€ΠΈ раскрытии оксиранового ΠΊΠΎΠ»ΡŒΡ†Π° ΠΏΠ΅Ρ€Π²ΠΈΡ‡Π½Ρ‹ΠΌΠΈ Π°ΠΌΠΈΠ½Π°ΠΌΠΈ, для Ρ€Π°ΡΡˆΠΈΡ€Π΅Π½ΠΈΡ ряда синтСтичСских ΠΏΡ€ΠΎΠΈΠ·Π²ΠΎΠ΄Π½Ρ‹Ρ… ΠΏΠΎΠ»ΠΈΠ°ΠΌΠΈΠ½ΠΎΠ², ΠΎΠ±Π»Π°Π΄Π°ΡŽΡ‰ΠΈΡ… ΠΏΡ€ΠΎΡ‚ΠΈΠ²ΠΎΠΎΠΏΡƒΡ…ΠΎΠ»Π΅Π²ΠΎΠΉ Π°ΠΊΡ‚ΠΈΠ²Π½ΠΎΡΡ‚ΡŒΡŽ.ΠœΠ΅Ρ‚ΠΎΠ΄Ρ‹. Π˜ΡΡ…ΠΎΠ΄Π½Ρ‹Π΅ соСдинСния – алкоголят Π³Π»ΠΈΡ†ΠΈΠ΄ΠΎΠ»Π° ΠΈΠ»ΠΈ эпихлоргидрин – Π²Π²ΠΎΠ΄ΠΈΠ»ΠΈ Π²ΠΎ взаимодСйствиС с гСксадСцилбромидом ΠΈΠ»ΠΈ гСксадСцилатом натрия, получая гСксадСцилглицидиловый эфир. ΠšΠ»ΡŽΡ‡Π΅Π²ΠΎΠΉ Ρ€Π΅Π°ΠΊΡ†ΠΈΠ΅ΠΉ получСния Π»ΠΈΠΏΠΎΡ„ΠΈΠ»ΡŒΠ½Ρ‹Ρ… ΠΏΠΎΠ»ΠΈΠ°ΠΌΠΈΠ½ΠΎΠ² являлось Π°ΠΌΠΈΠ½ΠΈΡ€ΠΎΠ²Π°Π½ΠΈΠ΅ Π»ΠΈΠΏΠΎΡ„ΠΈΠ»ΡŒΠ½Ρ‹Ρ… эпоксидов ΠΏΠΎΠ»ΠΈΠ°ΠΌΠΈΠ½Π°ΠΌΠΈ Π² присутствии Ρ‚Ρ€ΠΈΡ„Π»Π°Ρ‚Π° ΠΊΠ°Π»ΡŒΡ†ΠΈΡ. АцилированиС Π³ΠΈΠ΄Ρ€ΠΎΠΊΡΠΈΠ»ΡŒΠ½ΠΎΠΉ Π³Ρ€ΡƒΠΏΠΏΡ‹, ΠΎΠ±Ρ€Π°Π·ΠΎΠ²Π°Π²ΡˆΠ΅ΠΉΡΡ Π² Ρ…ΠΎΠ΄Π΅ раскрытия оксирана, ΠΏΡ€ΠΎΠ²ΠΎΠ΄ΠΈΠ»ΠΈ дСйствиСм 4-Π΄ΠΈΠΌΠ΅Ρ‚ΠΈΠ»Π°ΠΌΠΈΠ½ΠΎΠΏΠΈΡ€ΠΈΠ΄ΠΈΠ½Π° ΠΈ уксусного Π°Π½Π³ΠΈΠ΄Ρ€ΠΈΠ΄Π°. Π’Π²Π΅Π΄Π΅Π½ΠΈΠ΅ алкилильного замСститСля Π² присутствии Π³ΠΈΠ΄Ρ€ΠΈΠ΄Π° натрия ΠΏΡ€ΠΈΠ²ΠΎΠ΄ΠΈΠ»ΠΎ ΠΊ внутримолСкулярной Ρ†ΠΈΠΊΠ»ΠΈΠ·Π°Ρ†ΠΈΠΈ с ΠΎΠ±Ρ€Π°Π·ΠΎΠ²Π°Π½ΠΈΠ΅ΠΌ оксоазолидинового Ρ†ΠΈΠΊΠ»Π°. Π Π΅Π³ΠΈΠΎΡΠ΅Π»Π΅ΠΊΡ‚ΠΈΠ²Π½ΠΎΡΡ‚ΡŒ Ρ€Π΅Π°ΠΊΡ†ΠΈΠΈ раскрытия оксиранового Ρ†ΠΈΠΊΠ»Π° ΠΏΠΎ C(1) полоТСнию Π³Π»ΠΈΡ†Π΅Ρ€ΠΈΠ½Π° ΠΏΠΎΠ΄Ρ‚Π²Π΅Ρ€ΠΆΠ΄Π°Π»ΠΈ Π΄Π²ΡƒΠΌΠ΅Ρ€Π½ΠΎΠΉ гСтСроядСрной {1H,13C} спСктроскопиСй ядСрного ΠΌΠ°Π³Π½ΠΈΡ‚Π½ΠΎΠ³ΠΎ рСзонанса.Π Π΅Π·ΡƒΠ»ΡŒΡ‚Π°Ρ‚Ρ‹. Π Π°Π·Ρ€Π°Π±ΠΎΡ‚Π°Π½ ΠΈ Π°ΠΏΡ€ΠΎΠ±ΠΈΡ€ΠΎΠ²Π°Π½ ΠΏΠΎΠ΄Ρ…ΠΎΠ΄ ΠΊ синтСзу Π½ΠΎΠ²Ρ‹Ρ… Π»ΠΈΠΏΠΎΡ„ΠΈΠ»ΡŒΠ½Ρ‹Ρ… ΠΏΠΎΠ»ΠΈΠ°ΠΌΠΈΠ½ΠΎΠ², основанный Π½Π° каталитичСском Π°ΠΌΠΈΠ½ΠΈΡ€ΠΎΠ²Π°Π½ΠΈΠ΅ эпоксидов. ΠŸΠΎΠ»ΡƒΡ‡Π΅Π½Ρ‹ соСдинСния Π½Π° основС норспСрмина ΠΈ триэтилСнтСтрамина, содСрТащиС Π³ΠΈΠ΄Ρ€ΠΎΠΊΡΠΈΠ»ΡŒΠ½ΡƒΡŽ Π³Ρ€ΡƒΠΏΠΏΡƒ ΠΏΡ€ΠΈ Π‘(2) Π°Ρ‚ΠΎΠΌΠ΅ Π³Π»ΠΈΡ†Π΅Ρ€ΠΈΠ½ΠΎΠ²ΠΎΠ³ΠΎ остова. Для ΠΏΡ€ΠΎΠΈΠ·Π²ΠΎΠ΄Π½Ρ‹Ρ… норспСрмина ΠΏΡ€ΠΎΠ²Π΅Π΄Π΅Π½Π° модификация Π³ΠΈΠ΄Ρ€ΠΎΠΊΡΠΈΠ»ΡŒΠ½ΠΎΠΉ Π³Ρ€ΡƒΠΏΠΏΡ‹: Π²Π²Π΅Π΄Π΅Π½ Π°Ρ†Π΅Ρ‚ΠΈΠ»ΡŒΠ½Ρ‹ΠΉ Π·Π°ΠΌΠ΅ΡΡ‚ΠΈΡ‚Π΅Π»ΡŒ ΠΈ ΠΏΠΎΠ»ΡƒΡ‡Π΅Π½ΠΎ ΠΏΡ€ΠΎΠΈΠ·Π²ΠΎΠ΄Π½ΠΎΠ΅, содСрТащСС оксоазолидиновый Ρ†ΠΈΠΊΠ».Π’Ρ‹Π²ΠΎΠ΄Ρ‹. ΠŸΠΎΠ»ΡƒΡ‡Π΅Π½Π½Ρ‹Π΅ Π»ΠΈΠΏΠΎΡ„ΠΈΠ»ΡŒΠ½Ρ‹Π΅ ΠΏΠΎΠ»ΠΈΠ°ΠΌΠΈΠ½Ρ‹ ΠΌΠΎΠΆΠ½ΠΎ Ρ€Π°ΡΡΠΌΠ°Ρ‚Ρ€ΠΈΠ²Π°Ρ‚ΡŒ ΠΊΠ°ΠΊ ΠΏΠΎΡ‚Π΅Π½Ρ†ΠΈΠ°Π»ΡŒΠ½Ρ‹Π΅ ΠΏΡ€ΠΎΡ‚ΠΈΠ²ΠΎΠΎΠΏΡƒΡ…ΠΎΠ»Π΅Π²Ρ‹Π΅ Π°Π³Π΅Π½Ρ‚Ρ‹, для ΠΊΠΎΡ‚ΠΎΡ€Ρ‹Ρ… Π² дальнСйшСм Π±ΡƒΠ΄Π΅Ρ‚ ΠΏΡ€ΠΎΠ²Π΅Π΄Π΅Π½Π° ΠΎΡ†Π΅Π½ΠΊΠ° цитотоксичности ΠΏΡ€ΠΎΡ‚ΠΈΠ² Ρ€Π°Π·Π»ΠΈΡ‡Π½Ρ‹Ρ… Ρ€Π°ΠΊΠΎΠ²Ρ‹Ρ… ΠΊΠ»Π΅Ρ‚ΠΎΠΊ

    CK2 Inhibition and Antitumor Activity of 4,7-Dihydro-6-nitroazolo[1,5-a]pyrimidines

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    Today, cancer is one of the most widespread and dangerous human diseases with a high mortality rate. Nevertheless, the search and application of new low-toxic and effective drugs, combined with the timely diagnosis of diseases, makes it possible to cure most types of tumors at an early stage. In this work, the range of new polysubstituted 4,7-dihydro-6-nitroazolo[1,5-a]pyrimidines was extended. The structure of all the obtained compounds was confirmed by the data of 1H, 13C NMR spectroscopy, IR spectroscopy, and elemental analysis. These compounds were evaluated against human recombinant CK2 using the ADP-GloTM assay. In addition, the IC50 parameters were calculated based on the results of the MTT test against glioblastoma (A-172), embryonic rhabdomyosarcoma (Rd), osteosarcoma (Hos), and human embryonic kidney (Hek-293) cells. Compounds 5f, 5h, and 5k showed a CK2 inhibitory activity close to the reference molecule (staurosporine). The most potential compound in the MTT test was 5m with an IC50 from 13 to 27 Β΅M. Thus, our results demonstrate that 4,7-dihydro-6-nitroazolo[1,5-a]pyrimidines are promising for further investigation of their antitumor properties. Β© 2022 by the authors.Ministry of Education and Science of the Russian Federation,Β Minobrnauka: FEUZ-2020–0058,Β H687.42B.223/20This work was financially supported by the Ministry of Science and Higher Education of the Russian Federation, State Contract β„– FEUZ-2020–0058 (H687.42B.223/20)
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