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dc.date.accessioned | 2020-10-29T18:32:31Z | |
dc.date.available | 2020-10-29T18:32:31Z | |
dc.date.issued | 2019 | |
dc.identifier.uri | http://sedici.unlp.edu.ar/handle/10915/107975 | |
dc.description.abstract | In this investigation, we studied a family of compounds with an oxathiazolidine-4-one-2,2-dioxide skeleton and their amide synthetic precursors as new anticonvulsant drugs. The cyclic structures were synthesized using a three-step protocol that include solvent-free reactions and microwave-assisted heating. The compounds were tested in vivo through maximal electroshock seizure test in mice. All the structures showed activity at the lower doses tested (30 mg/Kg) and no signs of neurotoxicity were detected. Compound encoded as 1g displayed strong anticonvulsant effects in comparison with known anticonvulsants (ED50 = 29 mg/Kg). First approximations about the mechanisms of action of the cyclic structures were proposed by docking simulations and in vitro assays against sodium channels (patch clamp methods). | en |
dc.format.extent | 1465-1473 | es |
dc.language | en | es |
dc.subject | Epilepsy | es |
dc.subject | 1,2,3- oxathiazolidine-4-one-2,2- dioxide | es |
dc.subject | α-hydroxyimides | es |
dc.subject | docking | es |
dc.subject | sodium channels blockers | es |
dc.subject | MES test | es |
dc.subject | microwaveassisted synthesis | es |
dc.title | Design, synthesis and biological evaluation of N-substituted α-hydroxyimides and 1,2,3-oxathiazolidine-4-one-2,2-dioxides with anticonvulsant activity | en |
dc.type | Articulo | es |
sedici.identifier.uri | http://europepmc.org/backend/ptpmcrender.fcgi?accid=PMC6713207&blobtype=pdf | es |
sedici.identifier.uri | https://www.tandfonline.com/doi/full/10.1080/14756366.2019.1651722 | es |
sedici.identifier.other | pmid:31411081 | es |
sedici.identifier.other | pmcid:PMC6713207 | es |
sedici.identifier.other | doi:10.1080/14756366.2019.1651722 | es |
sedici.identifier.issn | 1475-6374 | es |
sedici.creator.person | Sabatier, Laureano Leonel | es |
sedici.creator.person | Palestro, Pablo Hernán | es |
sedici.creator.person | Enrique, Andrea Verónica | es |
sedici.creator.person | Pastore, Valentina | es |
sedici.creator.person | Sbaraglini, María Laura | es |
sedici.creator.person | Martín, Pedro | es |
sedici.creator.person | Gavernet, Luciana | es |
sedici.subject.materias | Ciencias Exactas | es |
sedici.description.fulltext | true | es |
mods.originInfo.place | Facultad de Ciencias Exactas | es |
mods.originInfo.place | Instituto de Estudios Inmunológicos y Fisiopatológicos | es |
sedici.subtype | Articulo | es |
sedici.rights.license | Creative Commons Attribution 4.0 International (CC BY 4.0) | |
sedici.rights.uri | http://creativecommons.org/licenses/by/4.0/ | |
sedici.description.peerReview | peer-review | es |
sedici.relation.journalTitle | Journal of Enzyme Inhibition and Medicinal Chemistry | es |
sedici.relation.journalVolumeAndIssue | vol. 34, no. 1 | es |