Synthesis and anticonvulsant activity of a class of 2-amino 3-hydroxypropanamide and 2-aminoacetamide derivatives
- GHIDINI E
- DELCANALE M
- DE FANTI R
- RIZZI A
- MAZZUFERI M.
- RODI D
- SIMONATO M
- LIPRERI M
- BASSANI F
- BATTIPAGLIA L
- BERGAMASCHI M
- VILLETTI G
DOIAbstract
Several studies have demonstrated that N-substituted aminoacid derivatives exhibit weak anticonvulsant activities in vivo. In the present study, a series of amides of aminoacids structurally related to aminoacetamide have been synthesised and investigated for anticonvulsant activity. Among the molecules investigated, those containing a bicyclic (tetralinyl, indanyl) group linked to the aminoacetamide chain (40, 47 and 59) were among the most active as anticonvulsants (ED50 > 10, <100 mg/kg after oral administration) against tonic seizures in the mouse maximal electroshock, bicuculline and picrotoxin tests at doses devoid of neurotoxic activity. Altogether, these results suggest the described compounds as a class of orally available anticonv...
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