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 / Maria Zappalà, Nicola Micale, Silvana Grasso, Frank S. Menniti, Giovambattista De Sarro, Carlo De Micheli. - In: ARKIVOC. - ISSN 1551-7004. - 2004(2004 Mar 10), pp. 196-203.
Titolo: | Synthesis of 1-substituted 3,5-dihydro-7,8-methylenedioxy-4H-2,3 benzodiazepin-4-ones as anticonvulsant agents | |
Autori: | ||
Parole Chiave: | 7,9-Dihydro-8H-[1,3]dioxolo[4,5-h][2,3]benzodiazepin-8-ones; anticonvulsant activity | |
Settore Scientifico Disciplinare: | Settore CHIM/08 - Chimica Farmaceutica | |
Data di pubblicazione: | 10-mar-2004 | |
Rivista: | ||
URL: | http://content.arkat-usa.org/ARKIVOC/JOURNAL_CONTENT/manuscripts/2004/VT-1018LP%20as%20published%20mainmanuscript.pdf | |
Tipologia: | Article (author) | |
Appare nelle tipologie: | 01 - Articolo su periodico |