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Isoindoline-1,3-dione Derivatives as Prototypes for Anticonvulsant Drug Discovery

dc.contributor.authorChelucci, Rafael Consolin [UNESP]
dc.contributor.authorChiquetto, Richard [UNESP]
dc.contributor.authorChiba, Diego Eidy [UNESP]
dc.contributor.authorScarim, Cauê Benito [UNESP]
dc.contributor.authorChin, Chung Man [UNESP]
dc.contributor.authordos Santos, Jean Leandro [UNESP]
dc.contributor.institutionUniversidade Estadual Paulista (UNESP)pt
dc.date.accessioned2026-07-24T13:33:21Z
dc.date.issued2025-01-09
dc.date.issued2025-01-01
dc.description.abstractINTRODUCTION: Epilepsy encompasses numerous syndromes characterized by spontaneous, intermittent, and abnormal electrical activity in the brain. Affecting about 1-2% of the population, it is estimated that approximately 30-40% of patients experience refractory epilepsy, which does not respond to traditional anticonvulsant drugs. AIMS: Therefore, developing novel, safe, and effective antiepileptic drugs remains a medical need. In this study, we synthesized a series of isoindoline-1,3-dione derivatives and evaluated their anticonvulsant effects. RESULTS: Compounds (2a-j) and (5) were obtained with yields ranging from 52-97%. These compounds were assessed for their protective effects on the following parameters: a) time to first seizure (seizure latency), b) seizure duration, and c) mortality rate post-seizure. The most active compound, (2a), increased seizure latency, reduced seizure duration, and lowered the mortality rate. CONCLUSION: These findings indicate that compound (2a) is a promising new anticonvulsant prototype, offering an alternative to current anticonvulsant drugs.
dc.description.abstractINTRODUCTION: Epilepsy encompasses numerous syndromes characterized by spontaneous, intermittent, and abnormal electrical activity in the brain. Affecting about 1-2% of the population, it is estimated that approximately 30-40% of patients experience refractory epilepsy, which does not respond to traditional anticonvulsant drugs. METHODS: Therefore, developing novel, safe, and effective antiepileptic drugs remains a medical need. In this study, we synthesized a series of isoindoline-1,3-dione derivatives and evaluated their anticonvulsant effects. RESULTS: Compounds (2a-j) and (5) were obtained with yields ranging from 52-97%. These compounds were assessed for their protective effects on the following parameters: a) time to first seizure (seizure latency), b) seizure duration, and c) mortality rate post-seizure. The most active compound, (2a), increased seizure latency, reduced seizure duration, and lowered the mortality rate. CONCLUSION: These findings indicate that compound (2a) is a promising new anticonvulsant prototype, offering an alternative to current anticonvulsant drugs.
dc.description.affiliationDepartment of Drugs and Medicines, School of Pharmaceutical Sciences, Sao Paulo State University-UNESP, Araraquara, Sao Paulo, Brazil
dc.description.affiliationUnespDepartment of Drugs and Medicines, School of Pharmaceutical Sciences, Sao Paulo State University-UNESP, Araraquara, Sao Paulo, Brazil
dc.identifierhttps://app.dimensions.ai/details/publication/pub.1184390353
dc.identifier.dimensionspub.1184390353
dc.identifier.doi10.2174/0115734064336758241113180402
dc.identifier.issn1573-4064
dc.identifier.issn1875-6638
dc.identifier.orcid0009-0008-4099-9986
dc.identifier.orcid0000-0003-2844-6402
dc.identifier.orcid0000-0002-2540-6395
dc.identifier.orcid0000-0003-4141-0455
dc.identifier.orcid0000-0002-2460-2829
dc.identifier.pmid39806977
dc.identifier.urihttps://hdl.handle.net/11449/328590
dc.publisherBentham Science Publishers
dc.relation.ispartofMedicinal Chemistry; n. 9; v. 21; p. 1000-1007
dc.rights.accessRightsAcesso restritopt
dc.rights.sourceRightsclosed
dc.sourceDimensions
dc.titleIsoindoline-1,3-dione Derivatives as Prototypes for Anticonvulsant Drug Discovery
dc.typeArtigopt
dspace.entity.typePublication
relation.isOrgUnitOfPublication95697b0b-8977-4af6-88d5-c29c80b5ee92
relation.isOrgUnitOfPublication.latestForDiscovery95697b0b-8977-4af6-88d5-c29c80b5ee92
unesp.campusUniversidade Estadual Paulista (UNESP), Faculdade de Ciências Farmacêuticas, Araraquarapt

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