Synthesis and pharmacological study of some new beta-(dialkylaminomethyl)- gamma-butyrolactones and their tetrahydrofuran analogues.

作者: Pouli N , Foscolos Gb , Fytas G , Vamvakides A , Marakos P

DOI:

关键词: Chemical synthesisConvulsantStimulationChemistryAnticonvulsantGlycine receptorStereochemistryLactoneTertiary amineNMDA receptor

摘要: This paper describes the synthesis of beta-(dialkylaminomethyl)-gamma- butyrolactones (6 and 15) their tetrahydrofuran analogs 7 16. Their convulsant activity was studied on mice could display an antiGABAergic component, but, unlike alpha-(dialkylaminomethyl)- gamma-butyrolactones, no antiglycinergic component detected. The possibility activation glutamatergic receptors (NMDA), by indirect stimulation glycinergic site, tetrahydrofurans be considered. These compounds exhibited, at low doses (1/3 to 1/20 doses), anticonvulsant action in maximal electroshock test this is agreement with abovementioned possibility.

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