Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1377847 | Bioorganic & Medicinal Chemistry Letters | 2006 | 4 Pages |
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.
Graphical abstractSynthesis, anticonvulsant activity and AMPA receptor affinity of 1-aryl-3,5-dihydro-7,8-ethylenedioxy-4H-2,3-benzodiazepin-4-ones (2a–f) are reported.Figure optionsDownload full-size imageDownload as PowerPoint slide