Synthesis and anticonvulsant activity of novel and potent 1-aryl-7,8-methylenedioxy-1,2,3,5-tetrahydro-4H-2,3-benzodiazepin-4-ones

The synthesis and anticonvulsant activity of 1-aryl-7,8-methylenedioxy-1,2, 3,5-tetrahydro-4H-2,3-benzodiazepin-4-(thi)ones (4a-d) and their 3-N-alkylc arbamoyl derivatives (4e-h) are reported. The new compounds possess marked anticonvulsant properties, comparable to those of the dehydro analogues 3 a nd higher than that of GYKI 52466 (1). Noteworthy, compound 4c shows a long er-lasting anticonvulsant activity. Electrophysiological experiments show t hat derivative 4c is less effective than 1 and 3c to reduce the KA-evoked c urrents in cerebellar granule neurons. (C) 2001 Elsevier Science Ltd. All r ights reserved.