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6-Amino quinazolinedione sulfonamides as orally active competitive AMPA receptor antagonists
Authors: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
Affiliation:Novartis Institute for Biomedical Research, Global Discovery Chemistry, Basel CH-4002, Switzerland. david.orain@novartis.com
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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