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Titolo:
Synthesis, anticonvulsant properties and pharmacokinetic profile of novel 10,11-dihydro-10-oxo-5H-dibenz/b,f/azepine-5-carboxamide derivatives
Autore:
Learmonth, DA; Benes, J; Parada, A; Hainzl, D; Beliaev, A; Bonifacio, MJ; Matias, PM; Carrondo, RLA; Garrett, J; Soares-da-Silva, P;
Indirizzi:
BIAL, Chem Lab, Dept Res & Dev, P-4785 S Mamede do Coronado, Portugal BIAL S Mamede do Coronado Portugal P-4785 S Mamede do Coronado, Portugal BIAL, Pharmacol Lab, Dept Res & Dev, P-4785 S Mamede do Coronado, PortugalBIAL S Mamede do Coronado Portugal P-4785 S Mamede do Coronado, Portugal Univ Nova Lisboa, Inst Tecnol Quim & Biol, P-2780 Oeiras, Portugal Univ Nova Lisboa Oeiras Portugal P-2780 & Biol, P-2780 Oeiras, Portugal
Titolo Testata:
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
fascicolo: 3, volume: 36, anno: 2001,
pagine: 227 - 236
SICI:
0223-5234(200103)36:3<227:SAPAPP>2.0.ZU;2-H
Fonte:
ISI
Lingua:
ENG
Soggetto:
SENSITIVE SODIUM-CHANNELS; CARBAMAZEPINE; DIPHENYLHYDANTOIN; METABOLISM; INHIBITION; BRAIN; DRUGS; CELLS;
Keywords:
anticonvulsant; dibenz/b,f/azepine-5-carboxamides; metabolism; sodium channel blockade; oxcarbazepine derivatives;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
25
Recensione:
Indirizzi per estratti:
Indirizzo: Soares-da-Silva, P BIAL, Chem Lab, Dept Res & Dev, P-4785 S Mamede do Coronado, Portugal BIAL S Mamede do Coronado Portugal P-4785 o, Portugal
Citazione:
D.A. Learmonth et al., "Synthesis, anticonvulsant properties and pharmacokinetic profile of novel 10,11-dihydro-10-oxo-5H-dibenz/b,f/azepine-5-carboxamide derivatives", EUR J MED C, 36(3), 2001, pp. 227-236

Abstract

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 8was 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 and5 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 issolely 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. (C) 2001 Editions scientifiques et medicales Elsevier SAS.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 06/04/20 alle ore 01:43:41