Isoindoline-1,3-dione Derivatives as Prototypes for Anticonvulsant Drug Discovery
| dc.contributor.author | Chelucci, Rafael Consolin [UNESP] | |
| dc.contributor.author | Chiquetto, Richard [UNESP] | |
| dc.contributor.author | Chiba, Diego Eidy [UNESP] | |
| dc.contributor.author | Scarim, Cauê Benito [UNESP] | |
| dc.contributor.author | Chin, Chung Man [UNESP] | |
| dc.contributor.author | dos Santos, Jean Leandro [UNESP] | |
| dc.contributor.institution | Universidade Estadual Paulista (UNESP) | pt |
| dc.date.accessioned | 2026-07-24T13:33:21Z | |
| dc.date.issued | 2025-01-09 | |
| dc.date.issued | 2025-01-01 | |
| dc.description.abstract | INTRODUCTION: 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.abstract | INTRODUCTION: 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.affiliation | Department of Drugs and Medicines, School of Pharmaceutical Sciences, Sao Paulo State University-UNESP, Araraquara, Sao Paulo, Brazil | |
| dc.description.affiliationUnesp | Department of Drugs and Medicines, School of Pharmaceutical Sciences, Sao Paulo State University-UNESP, Araraquara, Sao Paulo, Brazil | |
| dc.identifier | https://app.dimensions.ai/details/publication/pub.1184390353 | |
| dc.identifier.dimensions | pub.1184390353 | |
| dc.identifier.doi | 10.2174/0115734064336758241113180402 | |
| dc.identifier.issn | 1573-4064 | |
| dc.identifier.issn | 1875-6638 | |
| dc.identifier.orcid | 0009-0008-4099-9986 | |
| dc.identifier.orcid | 0000-0003-2844-6402 | |
| dc.identifier.orcid | 0000-0002-2540-6395 | |
| dc.identifier.orcid | 0000-0003-4141-0455 | |
| dc.identifier.orcid | 0000-0002-2460-2829 | |
| dc.identifier.pmid | 39806977 | |
| dc.identifier.uri | https://hdl.handle.net/11449/328590 | |
| dc.publisher | Bentham Science Publishers | |
| dc.relation.ispartof | Medicinal Chemistry; n. 9; v. 21; p. 1000-1007 | |
| dc.rights.accessRights | Acesso restrito | pt |
| dc.rights.sourceRights | closed | |
| dc.source | Dimensions | |
| dc.title | Isoindoline-1,3-dione Derivatives as Prototypes for Anticonvulsant Drug Discovery | |
| dc.type | Artigo | pt |
| dspace.entity.type | Publication | |
| relation.isOrgUnitOfPublication | 95697b0b-8977-4af6-88d5-c29c80b5ee92 | |
| relation.isOrgUnitOfPublication.latestForDiscovery | 95697b0b-8977-4af6-88d5-c29c80b5ee92 | |
| unesp.campus | Universidade Estadual Paulista (UNESP), Faculdade de Ciências Farmacêuticas, Araraquara | pt |

