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Название: | Evaluation of 5-[(Z)-(4-nitrobenzylidene)]-2-(thiazol-2-ylimino)- 4-thiazolidinone (Les-6222) as Potential Anticonvulsant Agent |
Авторы: | Shtrygol’, S. Mishchenko, M. Lozynskyi, A. Hoidyk, M. Khyluk, D. Gorbach, T. Lesyk, R. |
Ключевые слова: | antiepileptic drugs;thiazolidinones;pentylenetetrazole kindling;inflammation;molecular docking |
Дата публикации: | 2022 |
Библиографическое описание: | Evaluation of 5-[(Z)- (4-nitrobenzylidene)]-2-(thiazol-2- ylimino)-4-thiazolidinone (Les-6222) as Potential Anticonvulsant Agent / M. Mishchenko [et al.]. - Sci. Pharm. - 2022. - Vol. 90, Issue 56. |
Краткий осмотр (реферат): | 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 neuronspecific 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. |
URI (Унифицированный идентификатор ресурса): | http://dspace.nuph.edu.ua/handle/123456789/28524 |
Располагается в коллекциях: | Наукові публікації кафедри фармакологiї та фармакотерапії |
Файлы этого ресурса:
Файл | Описание | Размер | Формат | |
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Evaluation of 5-[(Z)-(4-nitrobenzylidene)]-2-(thiazol-2-ylimino))-4-thiazolidinone (Les-6222) as potential anticonvulsant agent.pdf | 1,45 MB | Adobe PDF | Просмотреть/Открыть |
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