6-Amino quinazolinedione sulfonamides as orally active competitive AMPA receptor antagonists
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Orain, David, Carcache, David, Froestl, Wolfgang, Allgeier, Hans, Rasetti, Vittorio, Nozulak, Joachim, Mattes, Henri, Koller, Manuel, Soldermann, Nicolas, Floersheim, Philipp, Desrayaud, Sandrine, Kallen, Joerg, Ofner, Silvio, 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 |