Синтез та алкілювання 6-(1H-бензімідазол-2-іл)-5-метилтієно[2,3-d]піримідин-4(3H)-онів

The one-step method for preparation of 6-(1H-benzimidazol-2-yl)-5-methylthieno[2,3-d]pyrimidin-4(3H)-ones by interaction of 5-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidine-6-carboxylic acid with ortho-pnenylediamines using 1,1’-carbonyldiimidazole as a coupling-reagent has been developed. The procedure proposed allows to obtain easily the target products using common reagents and solvents; and it also requires the simple isolation methods. The selectivity of 6-(1H-benzimidazol-2-yl)-5-methylthieno[2,3-d]pyrimidin-4(3H)-one interaction with benzyl chlorides in DMF – K2CO3 conditions has been studied using the NOESY spectroscopic method and alternative synthetic approaches; it has been determined that the reaction occurs at position 3 of the thieno[2,3-d] pyrimidine system. The study of the antimicrobial activity by the agar diffusion method for the compounds obtained has shown that 6-(1H-benzimidazol-2-yl)-3-benzyl-5-methylthieno[2,3-d]pyrimidin-4(3H)-ones reveal the antimicrobial activity against the strains of Escherichia coli, Proteus vulgaris, Pseudomonas aeruginosa; while the compound with unsubstituted position 3 appeared to be inactive against these strains of microorganisms. However, this compound exhibited the higher inhibitory activity against the Candida albicans fungi.Разработан эффективный одностадийный метод получения 6-(1H-бензимидазол-2-ил)-5-метилтиено [2,3-d]пиримидин-4(3H)-онов путем взаимодействия 5-метил-4-оксо-3,4-дигидротиено[2,3-d]пиримидин-6-карбоновой кислоты с орто-фенилендиаминами при использовании 1,1’-карбонилдиимидазола в качестве кaплинг-реагента. Данная методика позволяет легко получить конечные продукты при использовании простых реагентов и растворителей и требует стандартных методов выделения продукта. Исследовано направление реакции 6-(1H-бензимидазол-2-ил)-5-метилтиено[2,3-d]пиримидин-4(3H)-она с бензилхлоридами в условиях ДМФа – К2СО3, и с помощью данных спектроскопии NOESY и встречного синтеза установлено, что реакция протекает в положение 3 тиено[2,3-d]пиримидиновой системы. Изучение противомикробной активности полученных соединений методом диффузии в агар позволило установить, что 6-(1H-бензимидазол-2-ил)-3-бензил-5-метилтиено[2,3-d]пиримидин-4(3H)-оны проявяют противомикробную активность по отношению к таким штаммам микроорганизмов как Escherichia coli, Proteus vulgaris, Pseudomonas aeruginosa; в то же время незамещенное по положению 3 производное неактивно в отношении этих штаммов микроорганизмов. Однако, для незамещенного производного характерна чуть большая подавляющая активность в отношении грибов Candida albicans.Розроблено ефективний одностадійний метод одержання 6-(1H-бензімідазол-2-іл)-5-метилтієно[2,3-d] піримідин-4(3H)-онів шляхом взаємодії 5-метил-4-оксо-3,4-дигідротієно[2,3-d]піримідин-6-карбонової кислоти з орто-фенілендіамінами при використанні 1,1’-карбонілдіімідазолу в якості каплінг-реагента. Запропонована методика дозволяє легко одержувати кінцеві продукти при використанні простих реагентів і розчинників та вимагає стандартних методів виділення продукту. Досліджено напрям реакції 6-(1H-бензімідазол-2-іл)-5-метилтієно[2,3-d]піримідин-4(3H)-ону з бензилхлоридами в умовах ДМФа – К2СО3, та за допомогою даних спектроскопії NOESY і зустрічного синтезу встановлено, що дана реакція перебігає в положення 3 тієно[2,3-d]піримідинової системи. Дослідження антимікробної активності одержаних сполук методом дифузії в агар дозволило встановити, що 6-(1H-бензімідазол-2-іл)-3-бензил-5-метилтієно[2,3-d]піримідин-4(3H)-они виявляють антимікробну активність по відношенню до таких штамів мікроорганізмів як Escherichia coli, Proteus vulgaris, Pseudomonas aeruginosa, в той же час незаміщена по положенню 3 похідна неактивна по відношенню до цих штамів мікроорганізмів. Проте для незаміщеної похідної характерна дещо більша пригнічуюча активність по відношенню до грибів Candida albicans

Study of the time-differentiated particle flux density at various distances from EAS axis

The EAS time structure is studied using the enlarged EAS array of the Moscow State University. The time measurements are made using 22 scintillators which form 13 rectanges of 180x190 sq m size covering the entire array area. The array is triggered by a signal of 4-fold coincidences of the pulses from the detectors forming each of the rectangles. The data were obtained during 2200 hours of the array operation in 1984. A total of 816 showers, to which at least 14 of 22 scintillator detectors responded, were selected among all those detected. The coordinates of the EAS axis in the observation plane and the EAS sizes were determined by the maximum likelihood method using a computer on the assumption that the electron LDF is the NKG form. A total of 492 showers in the interval of EAS size Ne = 5x10 to the 6th power - 2x10 to the 8th power (N bar e = 1.7x 10 to the 7th power) with zenith angles theta or = 45 deg and axes within the array are analyzed

Методологія призначення індексу надійності для визначення технічного стану будівельних сталевих конструкцій

In order to assess the operational safety of steel constructions, the paper analyzes the principles of calculating the safety of structural steel constructions with consideration for the reliability index β at all phases of constructions operation and the design fundamentals of the reliability index β for both new constructions (at the design stage) and structural steel constructions in the conditions of the long-term operation.The task of safety and reliability calculations, first of all, consists in assigning normalized safety parameter values, i.e. normalizing the reliability index, the value of which should be strictly related to the consequence classes (CC), which are determining for setting the reliability coefficients for further calculations while designing the constructions.The article considers the calculation values β of the reliability index for constructions operated beyond the time limit for operation, with accumulated defects and damages. To improve the mechanism for calculating the reliability index value for the constructions operated beyond the maximum operating limit, with accumulated defects and damages, several tasks were set to determine such values β of the reliability index below which the construction is no longer considered to be operational and to define the reliability index values β for possible performance of renovation works (reconstruction, refurbishment) to strengthen and extend the remaining structural lifetime.Thus, emphasizing all of the aforementioned, the main conclusions to the article should be specified: at the stage of solving the issue of calculating the reliability index for structures being operated over the projected service life, with damages and initial defects accumulated during the operation period, it is required to perform their review and determine two main criteria for solving the issue of determining the reliability index, namely: to set such values of the reliability index below which the structure will be no longer operational, to define and set such values of the reliability index at which it is possible to carry out renovation works on steel structures, their reconstruction or repair. Considering the possibility of changing the reliability index compared to a new structure, given that the residual service life may be shorter than the design one, taking into account the economic factors and factors of probability of losing a person’s life, setting of such reliability index values is necessary for further possibility of the service life extension of a structure and determination of its residual life.У статті проаналізовано принципи розрахунків безпеки сталевих будівельних конструкцій з урахуванням індексу надійності b на всіх стадіях експлуатації конструкцій. Для оцінювання безпеки проаналізовані основні розрахункові положення індексу надійності для нових конструкцій (на стадії проектування) та для будівельних стальних конструкцій в умовах тривалої експлуатації

Arquivar atividades em termos de autenticidade de documentos eletrônicos e variação do número de cópias

The article is devoted to the problems of archive activity during the digital era, which are conditioned from the authors' point of view by the introduction of electronic documents that have changed the content of paperwork and archiving key categories - authenticity and copy number variation, as well as related originality and authenticity. The technologies of work in the archive, always considered as a unique system of originals are based on the traditional understanding of these categories. Using the method of expert assessments during the determination of key category content, the authors conclude that the current activity of the archives is aimed at copy production activity increase, their management and the provision of authenticity, reliability, integrity and suitability for use. Nowadays the issue of document archiving requires the consolidation of state and non-state structure efforts to develop a new attitude to the authenticity of electronic documents, to change the usual nature of archival institution interaction with users and interested citizens, state authorities and administration, law enforcement and judicial system.El artículo está dedicado a los problemas de la actividad de archivo durante la era digital, que están condicionados desde el punto de vista de los autores por la introducción de documentos electrónicos que han cambiado el contenido del papeleo y las categorías clave de archivo: autenticidad y variación del número de copias, como así como la originalidad y autenticidad relacionadas. Las tecnologías de trabajo en el archivo, siempre consideradas como un sistema único de originales, se basan en el entendimiento tradicional de estas categorías. Usando el método de evaluaciones de expertos durante la determinación del contenido de la categoría clave, los autores concluyen que la actividad actual de los archivos está dirigida a aumentar la actividad de producción de copias, su gestión y la provisión de autenticidad, confiabilidad, integridad y adecuación para su uso. Hoy en día, el tema del archivo de documentos requiere la consolidación de los esfuerzos de la estructura estatal y no estatal para desarrollar una nueva actitud hacia la autenticidad de los documentos electrónicos, para cambiar la naturaleza habitual de la interacción de la institución archivística con los usuarios y ciudadanos interesados, las autoridades estatales, la administración y la ley.O artigo é dedicado aos problemas da atividade de arquivo durante a era digital, eles são condicionados a partir do ponto de vista dos autores para a introdução de documentos eletrônicos que mudaram o conteúdo de documentos e categorias de arquivos-chave: autenticidade e variação do número de cópias, bem como a originalidade e autenticidade relacionadas. Tecnologias de trabalho no arquivo, sempre considerado como um único sistema original, com base no entendimento tradicional destas categorias. Usando o método de avaliações de peritos para a determinação da categoria-chave, os autores concluem que a atividade de arquivos atual visa aumentar cópias atividade de produção, gestão e prestação de autenticidade, confiabilidade, integridade e adequação para uso. Hoje, a questão do arquivamento de documentos requer a consolidação dos esforços de estruturas estatais e não-estatais para desenvolver uma nova atitude em relação à autenticidade dos documentos eletrônicos, para mudar a natureza habitual da interação da instituição de arquivo utilizadores e cidadãos interessados, autoridades estatais, administração e direito

Consistent alpha-cluster description of the 12C (0^+_2) resonance

The near-threshold 12C (0^+_2) resonance provides unique possibility for fast helium burning in stars, as predicted by Hoyle to explain the observed abundance of elements in the Universe. Properties of this resonance are calculated within the framework of the alpha-cluster model whose two-body and three-body effective potentials are tuned to describe the alpha - alpha scattering data, the energies of the 0^+_1 and 0^+_2 states, and the 0^+_1-state root-mean-square radius. The extremely small width of the 0^+_2 state, the 0_2^+ to 0_1^+ monopole transition matrix element, and transition radius are found in remarkable agreement with the experimental data. The 0^+_2-state structure is described as a system of three alpha-particles oscillating between the ground-state-like configuration and the elongated chain configuration whose probability exceeds 0.9

Methodological Approach to Evaluation of Individual Contribution of Specialists in Implementation of Administrative Consulting Projects

The article discusses the task of assessing the contribution of individual specialists working in the consulting services group. To date, such problems are solved mainly using the expert method. The article proposes a quantitative solution to this problem, based on the application of the mathematical apparatus of the theory of cooperative games and the theory of fuzzy set

Influence of frictional work on mine rail transport characteristics

В работе исследованы закономерности изменения эксплуатационных характеристик и фрикционных свойств пары колесо-рельс в зависимости от конструктивных и компоновочных параметров звеньев шахтного рельсового транспорта.An impact on exploitation and frictional characteristics of mining vehicle by means of variation of design scheme is studied. The study is provided depending on design and construction parameters of mining locomotive members

Giant Coulomb broadening and Raman lasing on ionic transitions

CW generation of anti-Stokes Raman laser on a number of blue-green argon-ion lines (4p-4s, 4p-3d) has been demonstrated with optical pumping from metastable levels 3d'^2G, 3d^4F. It is found, that the population transfer rate is increased by a factor of 3-5 (and hence, the output power of such Raman laser) owing to Coulomb diffusion in the velocity space. Measured are the excitation and relaxation rates for the metastable level. The Bennett hole on the metastable level has been recorded using the probe field technique. It has been shown that the Coulomb diffusion changes shape of the contour to exponential cusp profile while its width becomes 100 times the Lorentzian one and reaches values close to the Doppler width. Such a giant broadening is also confirmed by the shape of the absorption saturation curve.Comment: RevTex 18 pages, 5 figure

Influence of implantation of a novel domestic prosthetic aortic valve on the functional class of heart failure one year after surgery

Aim. To assess the severity of heart failure (HF) 1 year after aortic valve replacement with a novel bioprosthetic valve with the “easy change” system.Material and methods. The study included 59 patients (24 men and 35 women) diagnosed with degenerative aortic valve disease without concomitant cardiac pathology. The mean age of the patients was 69,6±4,3 years. An assessment of NYHA HF class using six-minute walk test was carried out. The venous plasma level of N-terminal pro-brain natriuretric peptide (NT-proBNP) before and after surgery was also used to determine the severity of HF. In 31 patients (52,5%), NYHA class III HF was determined before surgery.Results. Comparative analysis of HF classes revealed a significant difference. Thus, after implantation of MedEng-BIO prosthetic aortic valve, the distance of the six-minute walk test increased by an average of 125 m (p=0,001). NT-proBNP level decreased from 162,2 pg/ml to 63,7 pg/ml (p=0,003).Conclusion. One-year follow-up of patients after implantation of a novel bioprosthetic aortic valve showed an objective decrease in the severity of HF according to six-minute walk test and NT-proBNP level in venous blood plasma