5-(4-Aminobenzyl)-7,9-dihydro-8H-[1,3]dioxolo[4,5-h][2,3]benzodiazepin-8-one(3) and 7,9-dihydro-5-[2-(pyridin-2-yl)-vinyl]-8H-[1,3]dioxolo[4,5-h][2,3]benzodiazepin-8-one (4) were synthesized and screened as anticonvulsant agents in DBA/2 mice against sound-induced seizures. The new compounds are provided with anticonvulsant properties even if ED50 values are lower than those of prototype 5-(4-aminophenyl)-7,9-dihydro-8H-[1,3]dioxolo[4,5-h][2,3]benzodiazepin-8-one(2) and of GYKI 52466 (1), a well-known noncompetitive AMPA receptor antagonist. Binding assays and functional tests were performed to evaluate the affinity for AMPA and kainate receptors
Synthesis of 1-substituted 3,5-dihydro-7,8-methylenedioxy-4H-2,3 benzodiazepin-4-ones as anticonvulsant agents / M. Zappalà, N. Micale, S. Grasso, F.S. Menniti, G. De Sarro, C. DE MICHELI. - In: ARKIVOC. - ISSN 1551-7004. - 2004:(2004 Mar 10), pp. 196-203.
Synthesis of 1-substituted 3,5-dihydro-7,8-methylenedioxy-4H-2,3 benzodiazepin-4-ones as anticonvulsant agents
C. DE MICHELI
2004
Abstract
5-(4-Aminobenzyl)-7,9-dihydro-8H-[1,3]dioxolo[4,5-h][2,3]benzodiazepin-8-one(3) and 7,9-dihydro-5-[2-(pyridin-2-yl)-vinyl]-8H-[1,3]dioxolo[4,5-h][2,3]benzodiazepin-8-one (4) were synthesized and screened as anticonvulsant agents in DBA/2 mice against sound-induced seizures. The new compounds are provided with anticonvulsant properties even if ED50 values are lower than those of prototype 5-(4-aminophenyl)-7,9-dihydro-8H-[1,3]dioxolo[4,5-h][2,3]benzodiazepin-8-one(2) and of GYKI 52466 (1), a well-known noncompetitive AMPA receptor antagonist. Binding assays and functional tests were performed to evaluate the affinity for AMPA and kainate receptorsPubblicazioni consigliate
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.