Design, synthesis and biological evaluation of N-substituted α-hydroxyimides and 1,2,3-oxathiazolidine-4-one-2,2-dioxides with anticonvulsant activity.

Autor:	Sabatier, Laureano L., Palestro, Pablo H., Enrique, Andrea V., Pastore, Valentina, Sbaraglini, María L., Martín, Pedro, Gavernet, Luciana
Předmět:	BIOSYNTHESIS ANTICONVULSANTS SODIUM channels BIOCHEMICAL mechanism of action SEIZURES (Medicine) IN vivo studies
Zdroj:	Journal of Enzyme Inhibition & Medicinal Chemistry; Dec2019, Vol. 34 Issue 1, p1465-1473, 9p
Abstrakt:	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). [ABSTRACT FROM AUTHOR]
Databáze:	Complementary Index
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