220445-08-9Relevant academic research and scientific papers
2,3-benzodiazepine derivatives
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, (2008/06/13)
2,3-Benzodiazepines of formula (I), their stereoisomers and acid addition salts, wherein the variables have the meaning given in the specification, and pharmaceutical compositions containing them which are suitable for treating conditions associated with muscle spasms, epilepsy as well as acute and chronic forms of neurodegenerative diseases are disclosed.
New non competitive AMPA antagonists
Abraham, Gizella,Solyom, Sandor,Csuzdi, Emese,Berzsenyi, Pal,Ling, Istvan,Tarnawa, Istvan,Hamori, Tamas,Pallagi, Istvan,Horvath, Katalin,Andrasi, Ferenc,Kapus, Gabor,Harsing Jr., Laszlo G.,Kiraly, Istvan,Patthy, Miklos,Horvath, Gyula
, p. 2127 - 2143 (2007/10/03)
New halogen atom substituted 2,3-benzodiazepine derivatives condensed with an azole ring on the seven membered part of the ring system of type 3 and 4 as well as 5 and 6 were synthesized. It was found that chloro-, dichloro- and bromo-substitutions in the benzene ring and additionally imidazole ring condensation on the diazepine ring can successfully substitute the methylenedioxy group in the well known molecules GYKI 52466 (1) and GYKI 53773 (2) and the 3-acetyl-4-methyl structural feature in 2, respectively, preserving the highly active AMPA antagonist characteristic of the original molecules. From the most active compounds (3b,i) 3b (GYKI 47261) was chosen for detailed investigations. 3b revealed an excellent, broad spectrum anticonvulsant activity against seizures evoked by electroshock and different chemoconvulsive agents indicating a possible antiepileptic efficacy. 3b was found to be highly active in a transient model of focal ischemia predictive of a therapeutic value in human stroke. 3b also reversed the dopamine depleting effect of MPTP and antagonized the oxotremorine induced tremor in mice indicating a potential antiparkinson activity. Copyright (C) 2000 Elsevier Science Ltd.
