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Article

Evaluation of Anticonvulsant Activity of Dual COX-2/5-LOX Inhibitor Darbufelon and Its Novel Analogues

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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 Technology of Biologically Active Substances, Pharmacy and Biotechnology, Lviv Polytechnic National University,12 Bandery, 79013 Lviv, Ukraine
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Enamine Ltd., 23 Alexandra Matrosova, 01103 Kiev, Ukraine
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Department of Organic Chemistry and Pharmacy, Lesya Ukrainka Volyn National University, Volya Avenue 13, 43025 Lutsk, Ukraine
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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
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Author to whom correspondence should be addressed.
Academic Editor: Antoni Camins Espuny
Sci. Pharm. 2021, 89(2), 22; https://doi.org/10.3390/scipharm89020022
Received: 8 April 2021 / Revised: 14 May 2021 / Accepted: 18 May 2021 / Published: 19 May 2021
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. View Full-Text
Keywords: 4-thiazolidinones; darbufelone; dual COX-2/5-LOX inhibitor; pentylenetetrazole seizure; anticonvulsant activity 4-thiazolidinones; darbufelone; dual COX-2/5-LOX inhibitor; pentylenetetrazole seizure; anticonvulsant activity
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MDPI and ACS Style

Mishchenko, M.; Shtrygol’, S.; Lozynskyi, A.; Khomyak, S.; Novikov, V.; Karpenko, O.; Holota, S.; Lesyk, R. Evaluation of Anticonvulsant Activity of Dual COX-2/5-LOX Inhibitor Darbufelon and Its Novel Analogues. Sci. Pharm. 2021, 89, 22. https://doi.org/10.3390/scipharm89020022

AMA Style

Mishchenko M, Shtrygol’ S, Lozynskyi A, Khomyak S, Novikov V, Karpenko O, Holota S, Lesyk R. Evaluation of Anticonvulsant Activity of Dual COX-2/5-LOX Inhibitor Darbufelon and Its Novel Analogues. Scientia Pharmaceutica. 2021; 89(2):22. https://doi.org/10.3390/scipharm89020022

Chicago/Turabian Style

Mishchenko, Mariia; Shtrygol’, Sergiy; Lozynskyi, Andrii; Khomyak, Semen; Novikov, Volodymyr; Karpenko, Olexandr; Holota, Serhii; Lesyk, Roman. 2021. "Evaluation of Anticonvulsant Activity of Dual COX-2/5-LOX Inhibitor Darbufelon and Its Novel Analogues" Sci. Pharm. 89, no. 2: 22. https://doi.org/10.3390/scipharm89020022

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