%0 Journal Article
%T Design, synthesis and biological evaluation of N-substituted ¦Á-hydroxyimides and 1,2,3-oxathiazolidine-4-one-2,2-dioxides with anticonvulsant activity
%A Andrea V. Enrique
%A Laureano L. Sabatier
%A Luciana Gavernet
%A Mar¨ªa L. Sbaraglini
%A Pablo H. Palestro
%A Pedro Mart¨ªn
%A Valentina Pastore
%J Journal of Enzyme Inhibition and Medicinal Chemistry
%D 2019
%R https://doi.org/10.1080/14756366.2019.1651722
%X 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)
%U https://www.tandfonline.com/doi/full/10.1080/14756366.2019.1651722