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6-Amino quinazolinedione sulfonamides as orally active competitive AMPA receptor antagonists.
Orain, David; Ofner, Silvio; Koller, Manuel; Carcache, David A; Froestl, Wolfgang; Allgeier, Hans; Rasetti, Vittorio; Nozulak, Joachim; Mattes, Henri; Soldermann, Nicolas; Floersheim, Philipp; Desrayaud, Sandrine; Kallen, Joerg; Lingenhoehl, Kurt; Urwyler, Stephan.
Afiliação
  • Orain D; Novartis Institute for Biomedical Research, Global Discovery Chemistry, Basel CH-4002, Switzerland. david.orain@novartis.com
Bioorg Med Chem Lett ; 22(2): 996-9, 2012 Jan 15.
Article em En | MEDLINE | ID: mdl-22197388
ABSTRACT
A new set of quinazolinedione sulfonamide derivatives as competitive AMPA receptor antagonist with improved properties compared to 1 is disclosed. By modulating physico-chemical properties, compound 29 was identified with a low ED(50) of 5.5mg/kg in an animal model of anticonvulsant activity after oral dosage.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Sulfonamidas / Receptores de AMPA / Quinazolinonas / Anticonvulsivantes Limite: Animals Idioma: En Ano de publicação: 2012 Tipo de documento: Article
Texto completo
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Sulfonamidas / Receptores de AMPA / Quinazolinonas / Anticonvulsivantes Limite: Animals Idioma: En Ano de publicação: 2012 Tipo de documento: Article