80 research outputs found

    Solution of Euler-Type Non-Homogeneous Differential Equations with Three Fractional Derivatives

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    The linear non-homogeneous ordinary differential equations with three left-hand sided Lioville derivatives of fractional order are considered. Using the direct and inverse Mellin transforms and the residue theory, explicit solutions of such equations are established in terms of the generalized hypergeometric Wright functions, of the generalized hypergeometric functions and of the Euler psi function. The corresponding results are deduced for ordinary differential equations of Euler type. Examples are given. Mathematics Subject Classification: 34A05, 26A33, 44A99, 33C20, 33C99. Key Words and Phrases: linear differential equations with Liouville fractional derivatives, ordinary differential equations, explicit solutions, Mellin transforms, generalized Wright function, generalized hypergeometric function, Euler psi function

    Antidiabetogenic Features of Benzimidazoles

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    Literature data on the insulinogenic effect of 2-aminobenzimidazole prompted us to investigate its novel derivatives, particularly those containing an additional fused cycle in C1,2-α position, including imidazole, dihydroimidazole, or tetrahydropyrimidine ring. Consensus analysis of the hypoglycemic effect of these compounds performed with IT Microcosm and PASS system revealed that activity is mostly characteristic for N9-2,3-dihydroimidazo[1,2-a]benzimidazole derivatives. Substructural analysis of hypoglycemic activity identified substituents that determine the greatest pharmacological effect. According to the in silico assessment of the ADME properties, RU-254 was nominated as a lead compound due to the most optimal calculated and experimental activity and pharmacokinetic parameters. Preclinical studies have shown that identified compound has a pronounced insulinogenic effect and hypoglycemic effect, both in intact animals and in animals with experimental diabetes mellitus. RU-254 also reduces the level of glycated hemoglobin upon chronic administration, slightly decreases the activity of DPP-4, and increases the average number of Langerhans islets in the pancreas. Pharmaceutical drug formulation of RU-254 was developed and investigated for pharmacokinetic, pharmacodynamic, and toxicological properties. The dosage form of the drug under the name limiglidol (compound RU-254, diabenol) was evaluated in the full cycle of clinical studies that confirmed the safety, tolerability, and prominent antidiabetic properties of the drug

    Condensed Benzimidazoles Are a Novel Scaffold for Antioxidant Agents’ Search and Development

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    Taking into account that the imidazole ring has π-electron redundancy, condensed benzimidazole derivatives have attracted our attention as a promising class for the search for antioxidant substances. Synthesis was carried out, and information on the antioxidant activity of imidazo- and tetrahydropyrimido benzimidazoles was provided. Highly active antioxidant substance enoxifol has been revealed. The data on the synthesis and study of the pharmacodynamic, pharmacokinetic, and toxicological properties of the new antioxidant compound enoxifol are presented. The antioxidant activity of the compound is due to its ability to inactivate superoxide, hydroxyl, and peroxyl radicals, thereby reducing the overall oxidation rate due to a decrease in the total initiation rate. It has been shown that enoxifol has hepatoprotector, antihypoxic, cerebroprotective, nootropic, stress-protective, neuropsychotropic, actoprotective, cardioprotective, antiaggregant, and antithrombogenic properties and is able to prevent rheological disorders in diabetes mellitus

    Search for compounds with antioxidant and antiradical activity among N9-substituted 2-(biphenyl-4-yl)imidazo[1,2-a]benzimidazoles

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    The aim of this study was to synthesize and investigate in vitro antioxidant activity of promising novel compounds: 2-(biphenyl-4-yl)imidazo[1,2-a]benzimidazole

    Antiplatelet activity of new derivatives of benzimidazole containing sterically hindered phenolic group in their structure

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    The chemical class of benzimidazole derivatives with a hindered phenolic substituent in their structure is promising for the search for new antiaggregant and antioxidant drug

    Technology Platforms as an Efficient Tool to Modernize Russia's Economy

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    There is an urgent need to consider the dynamic development of the global economy from the point of view of its positive impact on competitiveness improvement in national manufacturing industries, and the best ways to modernize the country economy. The purpose of the paper is to provide with perspectives for development of instruments related to technology platforms within the framework of innovation management and adapted to the conditions of Russia's economic reality. The major method in studying this issue is mathematical economic modeling which has made it possible to facilitate expediency in determining a technology platform as an effective innovation control instrument.  The paper considers European and Russian experience in deploying technology platforms, and identifies national features characteristic to the performance of the innovation management instrument.  A mathematical economic model is used for justifying the efficiency of introducing technology platforms into Russian institutional innovation system. The practical significance of results and conclusions is in its ability to improve the mechanisms of developing and implementing federal and regional innovation development programs, development of the innovation infrastructure, stimulation of the innovation activity, use of a set of technology platform instruments by public authorities.  Keywords: technology platforms, innovative development, modernization, triple helix. JEL Classifications: C02, C18, O2

    Функционально замещенные сложные эфиры и диэфиры - производные селективно восстановленных безальдегидов ванилинового ряда

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    By selective reduction of vanillin-related benzaldehydes, using NaBH4 and Na [BH(OAc)3], the corresponding alcohols and diols have been synthesized. Their esterification by acyl chlorides in the presence of Et3N afforded functionally substituted esters and diesters containing fragments of heterocyclic compounds.Селективным восстановлением замещенных бензальдегидов ванилинового ряда с помощью NaBH4 или Na[BH(OAc)3] синтезированы спирты и диолы, их этерификацией хлорангидридами карбоновых кислот в присутствии Et3N получены функционально замещенные сложные эфиры и диэфиры, содержащие фрагменты гетероциклических соединений

    Синтез метиловых эфиров ( E, S)-2-арилиденамино-4-метилвалериановых кислот

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    By the reaction of L-leucine methyl ester hydrochloride with vanniline and vanillale ethers or esters, corresponding methyl esters of (Е,S)-2-arylidenamino-4-methylpentanoic acids have been synthesised.Конденсацией замещенных бензальдегидов ванилинового ряда с гидрохлоридом метилового эфира L-лейцина в присутствии гидрокарбоната натрия (при соотношении реагентов, равном 1:1:1) были синтезированы хиральные (Е,S)-алкилароматические азометины (основания Шиффа), содержащие простые и сложноэфирные группы

    Замещенные N-[изоксазол(изотиазол)-3-ил(метилен)метил]ариламины: синтез, комплексы с палладием и их каталитическая активность в водных средах

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    Schiff bases have been synthesized from substituted isoxazol- and isothiazol-3-carbaldehydes by condensation with biphenyl- and naphthyl amines. Reduction of azomethines obtained affords the corresponding amines. It has been shown that synthesized N-ligands form the palladium complexes possessing high catalytic activity in Suzuki reaction in aqueous and aqueous-alcohol media.Осуществлен молекулярный дизайн и выполнен синтез азометинов на основе замещенных изоксазол- и изотиазол-3-карбальдегидов по реакции с бифенил- и нафтиламинами. Установлено, что азометины образуются в виде Е-изомера. Восстановление полученных азометинов приводит к соответствующим аминам. Показано, что синтезированные N-лиганды образуют с хлоридом палладия комплексы, обладающие высокой каталитической активностью в реакции Сузуки в водной и водно-спиртовой средах. Реакции протекают с практически количественными выходами, что позволяет максимально упростить процедуру выделения целевых соединений. Введение карбоксильной группы в ароматический фрагмент для изоксазольных комплексов почти не влияет на каталитическую активность. В случае изотиазольных комплексов, каталитическая активность возрастает, причем эффект особенно хорошо заметен при 20оС

    Russian consensus statement on the diagnosis and treatment of patients with carotid stenosis

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    Carotid stenosis is a multidisciplinary problem that requires the involvement of a specialists’ team, including cardiovascular surgeons, neurosurgeons, endovascular surgeons, cardiologists, neurologists, and internists. In this consensus statement, a group of experts considered the main stages of diagnosing carotid stenosis, as well as discussed, the necessary prevention methods and features of choosing the optimal treatment approach. The aim was to provide concise and structured information on the management of patients with carotid stenosis. This document was developed based on the updated clinical guidelines of the European Society for Vascular Surgery and the American Association for Vascular Surgery, taking into account the consensus opinion of Russian experts
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