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6-Amino quinazolinedione sulfonamides as orally active competitive AMPA receptor antagonists

Orain, David and Carcache, David and Froestl, Wolfgang and Allgeier, Hans and Rasetti, Vittorio and Nozulak, Joachim and Mattes, Henri and Koller, Manuel and Soldermann, Nicolas and Floersheim, Philipp and Desrayaud, Sandrine and Kallen, Joerg and Ofner, Silvio and Lingenhoehl, Kurt and Urwyler, Stephan (2012) 6-Amino quinazolinedione sulfonamides as orally active competitive AMPA receptor antagonists. Bioorganic & Medicinal Chemistry Letters, 22 (2). pp. 996-999. ISSN 1464-3405

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 ED50 of 5.5 mg/kg in an animal model of anticonvulsant activity after oral dosage.

Item Type: Article
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Additional Information: Follow-up publication on the quinazolidione scaffold for AMPA. First publication was published earlier this year by Manuel Koller and coll.
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Date Deposited: 13 Oct 2015 13:14
Last Modified: 13 Oct 2015 13:14
URI: https://oak.novartis.com/id/eprint/6017

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