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http://dspace.nuph.edu.ua/handle/123456789/22587
Title: | Thiazole-bearing 4-thiazolidinones as new anticonvulsant agents |
Authors: | Mishchenko, M. V. Shtrygol', S. Yu. Kaminskyy, D. Lesyk, R. Мищенко, М. В. Міщенко, М. В. Штрыголь, С. Ю. Штриголь, С. Ю. Камінський, Д. Лесик, Р. |
Keywords: | 4-thiazolidinones;thiazoles;synthesis;anticonvulsant activity |
Issue Date: | 2020 |
Bibliographic description (Ukraine): | Thiazole-bearing 4-thiazolidinones as new anticonvulsant agents / M. Mishchenko, S. Shtrygol’, D. Kaminskyy, R. Lesyk // Sci. Pharm. – 2020. – Vol. 88, № 16. doi:10.3390/scipharm88010016 |
Abstract: | Here, we describe the synthesis and anticonvulsant activity of thiazole-bearing hybrids based on 2-imino-4-thiazolidinone and 2,4-dioxothiazolidine-5-carboxylic acid cores. The structure of target compounds was based on the following: (i) A combination of two thiazole cores; (ii) similarity to ralitolin’s structure; (iii) the compliance with structural requirements for the new anticonvulsants. Target compounds were synthesized via known approaches based on Knoenavegel reaction, alkylation reaction, and one-pot three-component reaction. Anticonvulsant properties of compounds were evaluated in two different models—pentylenetetrazole-induced seizures and maximal electroshock seizure tests. Among the tested compounds 5Z-(3-nitrobenzylidene)-2-(thiazol-2-ylimino)-thiazolidin-4-one Ib, 2-[2,4-dioxo-5-(thiazol-2- ylcarbamoylmethyl)-thiazolidin-3-yl]-N-(2-trifluoromethylphenyl)acetamide IId and (2,4-dioxo-5- (thiazol-2-ylcarbamoylmethylene)-thiazolidin-3-yl)acetic acid ethyl ester IIj showed excellent anticonvulsant activity in both models. The directions of compounds modification based on SAR aspects were discussed. The results of the study provide a basis for further study of the anticonvulsant properties of selected thiazole-thiazolidinones. |
URI: | http://dspace.nuph.edu.ua/handle/123456789/22587 |
Sponsorship: | none |
Appears in Collections: | Наукові видання кафедри фармакології та фармакотерапії |
Files in This Item:
File | Description | Size | Format | |
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Thiazole-Bearing 4-Thiazolidinones as New anticonvulsant agents.pdf | 987,81 kB | Adobe PDF | View/Open |
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