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-alkylcarbamoyl derivatives (4e-h) are reported. The new compounds possess marked anticonvulsant properties, comparable to those of the dehydro analogues 3 and higher than that of GYKI 52466 (1). Noteworthy, compound 4c shows a longer-lasting anticonvulsant activity. Electrophysiological experiments show that derivative 4c is less effective than 1 and 3c to reduce the KA-evoked currents in cerebellar granule neurons.
Dipartimento Farmaco-Chimico, Università di Messina, Italy. grasso@pharma.unime.it
S
S
Grasso
G
G
De Sarro
A
A
De Sarro
N
N
Micale
S
S
Polimeni
M
M
Zappalà
G
G
Puia
M
M
Baraldi
C
C
De Micheli
D000818:Animals; D014151:Anti-Anxiety Agents / Q000494:pharmacology; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology; D001569:Benzodiazepines; D051379:Mice; D008811:Mice, Inbred DBA; D018091:Receptors, AMPA / Q000037:antagonists & inhibitors*
D014151:Anti-Anxiety Agents; D000927:Anticonvulsants; D018091:Receptors, AMPA; C061950:GYKI 52466; D001569:Benzodiazepines