Synthesis and anticonvulsant properties of some 2-Aminoethanesulfonic acid (Taurine) derivatives

A series of 2‐acylaminoethanesulfonamides were synthesized by treating the corresponding sulfonyl chlorides with ammonia, a primary, or a secondary amine. A few compounds displayed marked anti‐convulsant activity in mice when tested for their potency in the maximal electroshock seizure test. The pip...

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Veröffentlicht in:Journal of pharmaceutical sciences 1984-01, Vol.73 (1), p.106-108
Hauptverfasser: Andersen, Lars, Sundman, Lars-Olav, Lindèn, Inge-Britt, Kontro, Pirjo, Oja, Simo S.
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Sprache:eng
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Zusammenfassung:A series of 2‐acylaminoethanesulfonamides were synthesized by treating the corresponding sulfonyl chlorides with ammonia, a primary, or a secondary amine. A few compounds displayed marked anti‐convulsant activity in mice when tested for their potency in the maximal electroshock seizure test. The piperidino, benzamido, phthalimido, and phenylsuccinylimido derivatives were active, whereas the succinylimido, saccharinylimido, and norbornendicarboxylimido compounds showed no activity. The interference with the sodium‐independent taurine binding to mouse brain synaptic membranes was assessed to elucidate the possible mode of anticonvulsant action.
ISSN:0022-3549
1520-6017
DOI:10.1002/jps.2600730128