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Your search keyword '"Ulomsky, E. N."' showing total 32 results
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32 results on '"Ulomsky, E. N."'

8. Oxidative Aromatization of 4,7-dihydro-6-nitroazolo[1,5-a] Pyrimidines: Synthetic Possibilities and Limitations, Mechanism of Destruction, and the Theoretical and Experimental Substantiation

Author

Lyapustin, D. N., Ulomsky, E. N., Balyakin, I. A., Shchepochkin, A. V., Rusinov, V. L., and Chupakhin, O. N.

Subjects
AZOLO[1,5-A]PYRIMIDINES, MULTICOMPONENT REACTIONS, SYNTHESIS OF HETEROCYCLES, NITRO COMPOUNDS, OXIDATION, OXIDATIVE DESTRUCTION, NITRO-SYNTHONS
Abstract

The reaction tolerance of the multicomponent process between 3-aminoazoles, 1-morpholino2-nitroalkenes, and aldehydes was studied. The main patterns of this reaction have been established. Conditions for the oxidation of 4,7-dihydro-6-nitroazolo[1,5-a]pyrimidines were selected. Previous claims that the 4,7-dihydro-6-nitroazolo[1,5-a]pyrimidines could not be aromatised have now been refuted. Compounds with an electron-donor substituent at position seven undergo decomposition during oxidation. The phenomenon was explained based on experimental data, electro-chemical experiment, and quantum-chemical calculation. The mechanism of oxidative degradation has been proposed. © 2021 by the authors. Licensee MDPI, Basel, Switzerland. Funding: The synthetic part was supported by the Ministry of Science and Higher Education of the Russian Federation, State Contract no FEUZ-2020-0058 (H687.42B.223/20). The electrochemical research and the quantum chemical calculations was funded by Russian Foundation for Basic Research (RFBR), project number 20-03-00814.

Published
2021

10. New antiglycating agents for diabetes therapy

Author

Savateev, K. V., Ulomsky, E. N., Rusinov, V. L., Chupakhin, O. N., Charushin, V. N., Sapozhnikova, I. M., Kotovskaya, S. K., Litvinov, R. A., Babkov, D. A., and Spasov, A. A.

Subjects
AZOLOPYRIMIDINES, ANTIGLYCATION, AZOLOTRIAZINES, ANTIDIABETIC, DIPEPTIDYL PEPTIDASE-4
Abstract

It was shown that azoloazines (1) demonstrated higher antiglycation activity than reference compound, aminoguanidine, and have some potential as dipeptidylpeptidase-4 inhibitors. By given results this class of heterocycles can be considered as candidate for extended studies to develop drugs against complications of T2DM [1-4]. The work was supported by the Ministry of Education and Science of Russia (grant №0836-2020-0058).

Published
2020

14. Azoloazines as Perspective Antiglycating Agents for Therapy of Diabetes Complications

Author

Savateev, K. V., Ulomsky, E. N., Rusinov, V. L., Chupakhin, O. N., Charushin, V. N., Sapozhnikova, I. M., Kotovskaya, S. K., Litvinov, R. A., Babkov, D. A., and Spasov, A. A.

Abstract

This work was supported by Russian Federation Ministry of education and science (grant № 4.6351.2017/8.9) and Russian Foundation for Basic Research (grant № 18-03-00787).

Published
2019

18. The features of nucleophilic substitution of the nitro group in 4-alkyl-6-nitro-1,2,4-triazolo[5,1-c][1,2,4]triazines

Author

Ulomsky, E. N., Lyapustin, D. N., Fedotov, V. V., El'tsov, O. S., Sapozhnikova, I. M., Kozhevnikov, D. N., and Mukhin, E. M.

Subjects
nucleophilic substitution, ANRORC, the transformation of 4-alkyl-6-nitro-1,2,4- triazolo[5,1-c][1,2,4]triazine-7-ones, morpholine, нуклеофильное замещение, превращение 4-алкил-6-нитро-4,7-дигидро-1,2,3-триазоло[5,1-с][1,2,4]триазин-7-онов, морфолин
Abstract

The nucleophilic substitution of the nitro group of 4-alkyl-6-nitro-4,7-dihydro-1,2,4-triazolo[5,1-c][1,2,4]triazine-7-ones on the example of interactionwith morpholine was studied. It is established that under the action of excess cycloalkylimine at room temperature the unusual easy disclosure of triazine cycle with the formation of sterically hindered hydrazones occurs which are the key intermediates for further transformations. The carrying of reaction at elevated temperatures leads to the formation of products of substitution of the nitro group with the amine and also with morpholyl hydrazones which are the products of hydrolysis of amides of hydrazones and subsequent decarboxylation. Thus, the nucleophilic substitution of the nitro group in the described triazolotriazines flows through the ANRORC mechanism., Исследовано нуклеофильное замещение нитрогруппы в 4-алкил-6-нитро-4,7-дигидро-1,2,3-триазоло[5,1-с][1,2,4]триазин-7-онах на примере взаимодействия с морфолином. Установлено, что под действием избытка циклоалкилимина при комнатной температуре происходит необычно легкое раскрытие триазинового цикла с образованием пространственно затрудненных гидразонов - ключевых интермедиатов для дальнейших превращений. Проведение реакции при повышенных температурах приводит к образованию продуктов замещения нитрогруппы амином, а также морфолилгидразонов - продуктов гидролиза амидов гидразонов и последующего декарбоксилирования. Таким образом, нуклеофильное замещение нитрогруппы в описанных триазолотриазинах протекает по механизму ANRORC.

Published
2017

19. Preparation of New 5-Methylthio-6-nitro-1,2,4-triazolo [1,5-a]pyrimidine-7-ones as Structural Analogues of Antiviral Drugs.

Author

Lyapustin, D. N., Ulomsky, E. N., Voinkov, E. K., and Rusinov, V. L.

Subjects
*PYRIMIDINES, *METHYL groups, *MOLECULAR structure, *ANTIVIRAL agents, *NITRATION
Abstract

Previously unknown nitroazolopyrimidines containing the methylsulfanyl group have beed synthesized. The nitration conditions not affecting the reactive methylsulfanyl group were selected. [ABSTRACT FROM AUTHOR]

Published
2019
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20. Cyanmorpholinoethylene in the Synthesis of Relevant Azoloazines.

Author

Fedotov, V. V., Savateev, K. V., Maltsev, M. A., Ulomsky, E. N., and Rusinov, V. L.

Subjects
AZO compound synthesis, ETHYLENE, PYRIMIDINES, AMINO group, CHEMICAL reactions, AZOLES
Abstract

Approach to the synthesis of promising azolopyrimidines containing a primary amino group by reactions of variously substituted aminoazoles with cyanmorpholinoethylene was developed. [ABSTRACT FROM AUTHOR]

Published
2019
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24. Azoloazines as A2a receptor antagonists. Structure-activity relationship

Author

Savateev, K V, Ulomsky, E N, Butorin, I I, Charushin, V N, Rusinov, V L, and Chupakhin, O N

Abstract

Non-xanthine inhibitors of the adenosine A2a receptor of the azoloazine series are good candidates for use as drugs for the treatment of neurodegenerative diseases and sepsis. This review systematizes and summarizes the structure-activity relationships in the series of triazoloazines, including annulated pyrimidines, pyrazines and triazines, as well as their tricyclic fused analogues. The above relationships for such systems are analyzed. The structures of the most efficient functional moieties from the point of view of affinity for the A2a receptor and selectivity for other types of adenosine receptors (A1, A2b, A3) are presented. The bibliography includes 71 references.

Published
2018

27. New Approach to the Synthesis of Azauracils and Azaisocytosines.

Author

Shestakova, T. S., primary, Deev, S. L., additional, Ulomsky, E. N., additional, Rusinov, V. L., additional, Chupakhin, O. N., additional, D'yachenko, O. A., additional, Kazheva, O. N., additional, Chekhlov, A. N., additional, Slepukhin, P. A., additional, and Kodess, M. I., additional

Published
2007
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32. [Investigation of Therapeutic Efficacy of Triazavirin Against Experimental Forest-Spring Encephalitis on Albino Mice].

Author

Loginova SY, Borisevich SV, Rusinov VL, Ulomsky EN, Charushin VN, Chupakhin ON, and Sorokin PV

Subjects
Animals, Brain drug effects, Brain pathology, Brain virology, Encephalitis Viruses, Tick-Borne pathogenicity, Encephalitis Viruses, Tick-Borne physiology, Encephalitis, Tick-Borne mortality, Encephalitis, Tick-Borne pathology, Encephalitis, Tick-Borne virology, Mice, Ribavirin pharmacology, Survival Analysis, Treatment Outcome, Triazoles, Viral Load drug effects, Antiviral Agents pharmacology, Azoles pharmacology, Encephalitis Viruses, Tick-Borne drug effects, Encephalitis, Tick-Borne drug therapy, Triazines pharmacology, Virus Replication drug effects
Abstract

The comparative study of the therapeutic efficacy of Triazavirin against experimental Forest-Spring encephalitis on albino mice vs. the active drug Ribavirin® showed that in high doses (200-400 mg/kg) Triazavirin moderately protected the infected animals. A significant increase of the animal lifespan in the test groups (from 4.1 to 4.8 days) and a statistically (p ≤ 0.05) valid decrease of the virus accumulation in the target organ (the brain) were observed.

Published
2015

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