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Open AccessArticle

Thiazole-Bearing 4-Thiazolidinones as New Anticonvulsant Agents

1
Department of Pharmacology, National University of Pharmacy, Kulykovska 12, 61168 Kharkiv, Ukraine
2
Department of Pharmaceutical, Organic and Bioorganic Chemistry, Danylo Halytsky Lviv National Medical University, Pekarska 69, 79010 Lviv, Ukraine
3
Department of Public Health, Dietetics and Lifestyle Disorders, Faculty of Medicine, University of Information Technology and Management in Rzeszow, Sucharskiego 2, 35-225 Rzeszow, Poland
*
Author to whom correspondence should be addressed.
Sci. Pharm. 2020, 88(1), 16; https://doi.org/10.3390/scipharm88010016
Received: 19 February 2020 / Revised: 10 March 2020 / Accepted: 18 March 2020 / Published: 24 March 2020
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. View Full-Text
Keywords: 4-thiazolidinones; thiazoles; synthesis; anticonvulsant activity 4-thiazolidinones; thiazoles; synthesis; anticonvulsant activity
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Mishchenko, M.; Shtrygol, S.; Kaminskyy, D.; Lesyk, R. Thiazole-Bearing 4-Thiazolidinones as New Anticonvulsant Agents. Sci. Pharm. 2020, 88, 16.

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