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http://dspace.nuph.edu.ua/handle/123456789/25772
Title: | Evaluation of anticonvulsant activity of dual COX-2/5-LOX inhibitor darbufelon and its novel analogues |
Authors: | Mishchenko, M. Shtrygol’, S. Lozynskyi, A. Khomyak, S. Novikov, V. Karpenko, O. Holota, S. Lesyk, R. |
Keywords: | 4-thiazolidinones;darbufelone;dual COX-2/5-LOX inhibitor;pentylenetetrazole seizure;anticonvulsant activity |
Issue Date: | 2021 |
Bibliographic description (Ukraine): | Evaluation of anticonvulsant activity of dual COX-2/5-LOX inhibitor darbufelon and its novel analogues / Mariia Mishchenko [et al.] // Sci. Pharm. - 2021. - 89 (2). |
Abstract: | Neuroinflammation is an integral part of epilepsy pathogenesis and other convulsive conditions, and non-steroidal anti-inflammatory drugs (NSAIDs) present a potent tool for the contemporary search and design of novel anticonvulsants. In the present paper, evaluation of the anticonvulsant activity of the potential NSAID dual COX-2/5-LOX inhibitor darbufelone methanesulfonate using an scPTZ model in mice in dose 100 mg/kg is reported. Darbufelone possesses anticonvulsant properties in the scPTZ model and presents interest for in-depth studies as a possible anticonvulsant multi-target agent with anti-inflammatory activity. The series of 4-thiazolidinone derivatives have been synthesized following the analogue-based drug design and hybrid-pharmacophore approach using a darbufelone matrix. The synthesized derivatives showed a significant protection level for animals in the scPTZ model and are promising compounds for the design of potential anticonvulsants with satisfactory drug-like parameters. |
URI: | http://dspace.nuph.edu.ua/handle/123456789/25772 |
Appears in Collections: | Наукові публікації кафедри фармакологiї та фармакотерапії |
Files in This Item:
File | Description | Size | Format | |
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Evaluation of Anticonvulsant Activity of Dual COX-2-5-LOXInhibitor Darbufelon and Its Novel Analogues.pdf | 1,8 MB | Adobe PDF | View/Open |
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