A series of 1-aryl-3,5-dihydro-7,8-ethylenedioxy-4H-2,3-benzodiazepin-4-ones 2a-f, were synthesized and screened as anticonvulsant agents in DBA/2 mice against sound-induced seizures. The new compounds display anticonvulsant properties although the ED50 values are higher than those of prototypes 1-aryl-3,5-dihydro-7,8-methylenedioxy-4H-2.3-benzodiazepin-4-ones (1) and GYKI 52466, well-known noncompetitive AMPA receptor antagonists. Functional tests were performed to evaluate the antagonistic activity at the AMPA and kainate receptors
New 7,8-ethylenedioxy-2,3-benzodiazepines as noncompetitive AMPA receptor antagonists / Maria Zappalà, Alessia Pellicanò, Nicola Micale, Frank S. Menniti, Guido Ferreri, Giovambattista De Sarro, Silvana Grasso, Carlo De Micheli. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 16:1(2006), pp. 167-170.
New 7,8-ethylenedioxy-2,3-benzodiazepines as noncompetitive AMPA receptor antagonists
Carlo De Micheli
2006
Abstract
A series of 1-aryl-3,5-dihydro-7,8-ethylenedioxy-4H-2,3-benzodiazepin-4-ones 2a-f, were synthesized and screened as anticonvulsant agents in DBA/2 mice against sound-induced seizures. The new compounds display anticonvulsant properties although the ED50 values are higher than those of prototypes 1-aryl-3,5-dihydro-7,8-methylenedioxy-4H-2.3-benzodiazepin-4-ones (1) and GYKI 52466, well-known noncompetitive AMPA receptor antagonists. Functional tests were performed to evaluate the antagonistic activity at the AMPA and kainate receptorsPubblicazioni consigliate
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