Antioxidant Activity of Quinoxalyl Hydrazones of 2-Hydroxyimino-1,3-dicarbonyl Compounds

Biosimilarity and pharmacokinetic descriptors were obtained using SwissADME and ADMETlab 2.0 web services. Analysis of the obtained descriptors shows that, according to Lipinski's rule, quinoxalyl hydrazones of 2-hydroximino-1,3-dioxocompounds may be promising candidates for drug development fo...

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Κύριοι συγγραφείς:	Anenko, D. S., Аненко, Д. С., Glizhova, T. N., Глижова, Т. Н.
Μορφή:	Статья
Γλώσσα:	English
Έκδοση:	2024
Θέματα:	Antioxidant activity Quinoxalyl hydrazones of 2-hydroxyimino-1,3-dicarbonyl compounds
Διαθέσιμο Online:	https://dspace.ncfu.ru/handle/20.500.12258/26895
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spelling	ir-20.500.12258-268952024-03-07T08:48:27Z Antioxidant Activity of Quinoxalyl Hydrazones of 2-Hydroxyimino-1,3-dicarbonyl Compounds Anenko, D. S. Аненко, Д. С. Glizhova, T. N. Глижова, Т. Н. Antioxidant activity Quinoxalyl hydrazones of 2-hydroxyimino-1,3-dicarbonyl compounds Biosimilarity and pharmacokinetic descriptors were obtained using SwissADME and ADMETlab 2.0 web services. Analysis of the obtained descriptors shows that, according to Lipinski's rule, quinoxalyl hydrazones of 2-hydroximino-1,3-dioxocompounds may be promising candidates for drug development for oral administration. Analysis of the pharmacokinetic descriptors of the structures studied shows that, according to the in silico predictions, the compounds can penetrate the blood-brain barrier, be absorbed in the gastrointestinal tract, bind to plasma proteins, be rapidly eliminated from target cells and inhibit CYP3A4, CYP1A2, CYP2C19 and CYP2D6 isoenzymes. The antioxidant activity of quinoxalyl hydrazone derivatives with different benzoyl, ester and acetyl moieties has been studied. Pharmacological screening of the obtained compounds was performed in vitro in the model of Fe2+-induced lipid peroxidation. The data of pharmacological screening indicate clearly pronounced inhibition of lipid peroxidation in the system of yolk lipoproteins by the compounds obtained, which indicates a significant contribution of quinoxalone scaffold in the manifestation of antioxidant properties. Variations in the structure of the starting 1,3-dicarbonyl compounds did not result in significant changes in the antioxidant activity of the obtained hydrazones. The compounds obtained can be promising compounds with marked antioxidant activity for further in vivo studies, including investigation of acute and chronic toxicity. The leading compound is tolyl-substituted quinoxalyl hydrazone IIb. 2024-03-07T08:46:41Z 2024-03-07T08:46:41Z 2023 Статья Anenko, DS; Bobrov, PS; Abisalova, IL; Suboch, GA; Sergeeva, EO; Glizhova, TN. Antioxidant Activity of Quinoxalyl Hydrazones of 2-Hydroxyimino-1,3-dicarbonyl Compounds // CHEMISTRY FOR SUSTAINABLE DEVELOPMENT. - 2023. - 31(4). - рр. 349-353. - DOI: 10.15372/CSD2023477 http://hdl.handle.net/20.500.12258/26895 en CHEMISTRY FOR SUSTAINABLE DEVELOPMENT application/pdf
institution	СКФУ
collection	Репозиторий
language	English
topic	Antioxidant activity Quinoxalyl hydrazones of 2-hydroxyimino-1,3-dicarbonyl compounds
spellingShingle	Antioxidant activity Quinoxalyl hydrazones of 2-hydroxyimino-1,3-dicarbonyl compounds Anenko, D. S. Аненко, Д. С. Glizhova, T. N. Глижова, Т. Н. Antioxidant Activity of Quinoxalyl Hydrazones of 2-Hydroxyimino-1,3-dicarbonyl Compounds
description	Biosimilarity and pharmacokinetic descriptors were obtained using SwissADME and ADMETlab 2.0 web services. Analysis of the obtained descriptors shows that, according to Lipinski's rule, quinoxalyl hydrazones of 2-hydroximino-1,3-dioxocompounds may be promising candidates for drug development for oral administration. Analysis of the pharmacokinetic descriptors of the structures studied shows that, according to the in silico predictions, the compounds can penetrate the blood-brain barrier, be absorbed in the gastrointestinal tract, bind to plasma proteins, be rapidly eliminated from target cells and inhibit CYP3A4, CYP1A2, CYP2C19 and CYP2D6 isoenzymes. The antioxidant activity of quinoxalyl hydrazone derivatives with different benzoyl, ester and acetyl moieties has been studied. Pharmacological screening of the obtained compounds was performed in vitro in the model of Fe2+-induced lipid peroxidation. The data of pharmacological screening indicate clearly pronounced inhibition of lipid peroxidation in the system of yolk lipoproteins by the compounds obtained, which indicates a significant contribution of quinoxalone scaffold in the manifestation of antioxidant properties. Variations in the structure of the starting 1,3-dicarbonyl compounds did not result in significant changes in the antioxidant activity of the obtained hydrazones. The compounds obtained can be promising compounds with marked antioxidant activity for further in vivo studies, including investigation of acute and chronic toxicity. The leading compound is tolyl-substituted quinoxalyl hydrazone IIb.
format	Статья
author	Anenko, D. S. Аненко, Д. С. Glizhova, T. N. Глижова, Т. Н.
author_facet	Anenko, D. S. Аненко, Д. С. Glizhova, T. N. Глижова, Т. Н.
author_sort	Anenko, D. S.
title	Antioxidant Activity of Quinoxalyl Hydrazones of 2-Hydroxyimino-1,3-dicarbonyl Compounds
title_short	Antioxidant Activity of Quinoxalyl Hydrazones of 2-Hydroxyimino-1,3-dicarbonyl Compounds
title_full	Antioxidant Activity of Quinoxalyl Hydrazones of 2-Hydroxyimino-1,3-dicarbonyl Compounds
title_fullStr	Antioxidant Activity of Quinoxalyl Hydrazones of 2-Hydroxyimino-1,3-dicarbonyl Compounds
title_full_unstemmed	Antioxidant Activity of Quinoxalyl Hydrazones of 2-Hydroxyimino-1,3-dicarbonyl Compounds
title_sort	antioxidant activity of quinoxalyl hydrazones of 2-hydroxyimino-1,3-dicarbonyl compounds
publishDate	2024
url	https://dspace.ncfu.ru/handle/20.500.12258/26895
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Antioxidant Activity of Quinoxalyl Hydrazones of 2-Hydroxyimino-1,3-dicarbonyl Compounds

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