461670-31-5Relevant academic research and scientific papers
Synthesis, anticonvulsant properties and pharmacokinetic profile of novel 10,11-dihydro-10-oxo-5H-dibenz/b,f/azepine-5-carboxamide derivatives
Learmonth, David A,Benes, Jan,Parada, Antonio,Hainzl, Dominik,Beliaev, Alexander,Bonifacio, Maria Joao,Matias, Pedro M,Carrondo, Maria A,Garrett, Jose,Soares-Da-Silva, Patricio
, p. 227 - 236 (2001)
A series of novel derivatives of oxcarbazepine (5), 10,11-dihydro-10-oxo-5H-dibenz/b,f/azepine-5-carboxamide was synthesised and evaluated for their anticonvulsant activity and sodium channel blocking properties. The oxime 8 was found to be the most active compound from this series, displaying greater potency than its geometric isomer 9 and exhibiting also the highest protective index value. Importantly, the metabolic profile of 8 differs from the already established dibenz/b,f/azepine-5-carboxamide drugs such as 1 and 5 which undergo rapid and complete conversion in vivo to several biologically active metabolites. In contrast 8 is metabolised to only a very minor extent leading to the conclusion that the observed anti-convulsant effect is solely attributable to 8. It is concluded that 8 may be as effective as 1 and 5 at controlling seizures and that the low toxicity and consequently high protective index should provide the compound with an improved side-effect profile.
Derivatives of 10, 11-Dihydro-10-OXO-5H-Dibenz/B,F/Azepine-5-carboxamide
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, (2008/06/13)
Compounds of general formula I are described STR1 as is a process for their preparation which consists of reacting a compound of formula II STR2 with hydroxylamine or its derivatives of formula III The compounds cited in the present invention have valuable pharmaceutical properties namely in the treatment of some disturbances in the central and peripheral nervous system.
Derivatives of 10,11-dihydro-10-oxo-5h-dibenz/b,f/azepine-5-carboxamide
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, (2008/06/13)
Compounds of general formula I are described as is a process for their preparation which consists of reacting a compound of formula II with hydroxylamine or its derivatives of formula III H2NOR2The compounds cited in the present inve
