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Article

Evaluation of 5-[(Z)-(4-nitrobenzylidene)]-2-(thiazol-2-ylimino)-4-thiazolidinone (Les-6222) as Potential Anticonvulsant Agent

1
Department of Pharmacology and Pharmacotherapy, National University of Pharmacy, 53 Pushkinska, 61002 Kharkiv, Ukraine
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Department of Pharmaceutical, Organic and Bioorganic Chemistry, Danylo Halytsky Lviv National Medical University, 69 Pekarska, 79010 Lviv, Ukraine
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Department of Organic Chemistry, Medical University of Lublin, Aleje Racławickie 1, 20-059 Lublin, Poland
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Department of Biological Chemistry, Kharkiv National Medical University, 4 Nauky Ave, 61022 Kharkiv, Ukraine
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Department of Biotechnology and Cell Biology, Medical College, University of Information Technology and Management in Rzeszow, Sucharskiego 2, 35-225 Rzeszow, Poland
*
Author to whom correspondence should be addressed.
Academic Editor: Valentina Onnis
Sci. Pharm. 2022, 90(3), 56; https://doi.org/10.3390/scipharm90030056
Received: 1 August 2022 / Revised: 26 August 2022 / Accepted: 1 September 2022 / Published: 19 September 2022
(This article belongs to the Special Issue Heterocyclic Chemistry in Drug Design 2.0)
It was determined that the studied 5-[(Z)-(4-nitrobenzylidene)]-2-(thiazol-2-ylimino)-4-thiazolidinone (Les-6222) affects the cyclooxygenase pathway of the arachidonic acid cascade, the markers of damage to neurons on models of PTZ kindling. In the model of chronic epileptogenesis in mice (pentylenetetrazole kindling), a 4-thiazolidinone derivative showed high anticonvulsant activity, which is weaker than the effect of sodium valproate and higher than Celecoxib. The mentioned compound has a pronounced anti-inflammatory effect in the brain on the background of the PTZ kindling, reliably inhibiting COX-1 and COX-2. The predominant inhibition of COX-2 by 44.5% indicates this enzyme’s high selectivity of Les-6222. According to the molecular docking study results, the studied compound revealed the properties of COX-1/COX-2 inhibitor and especially 5-LOX/FLAP. The decreasing content of 8-isoprostane in the brain of mice of the Les-6222 group indicates a beneficial effect on cell membranes in the background of oxidative stress during the long-term administration of PTZ. In addition, Les-6222 significantly decreased the content of neuron-specific enolase, indicating neuroprotective properties in the background of chronic epileptogenesis. The obtained results experimentally substantiate the feasibility of further developing Les-6222 as a promising anticonvulsant agent. View Full-Text
Keywords: antiepileptic drugs; thiazolidinones; pentylenetetrazole kindling; inflammation; molecular docking antiepileptic drugs; thiazolidinones; pentylenetetrazole kindling; inflammation; molecular docking
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MDPI and ACS Style

Mishchenko, M.; Shtrygol’, S.; Lozynskyi, A.; Hoidyk, M.; Khyluk, D.; Gorbach, T.; Lesyk, R. Evaluation of 5-[(Z)-(4-nitrobenzylidene)]-2-(thiazol-2-ylimino)-4-thiazolidinone (Les-6222) as Potential Anticonvulsant Agent. Sci. Pharm. 2022, 90, 56. https://doi.org/10.3390/scipharm90030056

AMA Style

Mishchenko M, Shtrygol’ S, Lozynskyi A, Hoidyk M, Khyluk D, Gorbach T, Lesyk R. Evaluation of 5-[(Z)-(4-nitrobenzylidene)]-2-(thiazol-2-ylimino)-4-thiazolidinone (Les-6222) as Potential Anticonvulsant Agent. Scientia Pharmaceutica. 2022; 90(3):56. https://doi.org/10.3390/scipharm90030056

Chicago/Turabian Style

Mishchenko, Mariia, Sergiy Shtrygol’, Andrii Lozynskyi, Mykhailo Hoidyk, Dmytro Khyluk, Tatyana Gorbach, and Roman Lesyk. 2022. "Evaluation of 5-[(Z)-(4-nitrobenzylidene)]-2-(thiazol-2-ylimino)-4-thiazolidinone (Les-6222) as Potential Anticonvulsant Agent" Scientia Pharmaceutica 90, no. 3: 56. https://doi.org/10.3390/scipharm90030056

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