NOVELES AMIDAS Y HETEROCICLOS CON ACTIVIDAD ANTICONVULSIVA.

ENRIQUE, ANDREA; GAVERNET, LUCIANA; PALESTRO, PABLO; MARTÍN, PEDRO; SABATIER, LAUREANO LEONEL; PASTORE, VALENTINA

BUENOS AIRES

Congreso; XXXII Congreso Argentino de Química; 2019

AQA

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).