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Design and synthesis of Selurampanel, a novel orally active and competitive AMPA receptor antagonist.

Mattes, Henri and Orain, David and Tasdelen, Engin and Haessig, Samuel and Koller, Manuel and Picard, Anne and Dubois, Celine and Lingenhoehl, Kurt and Desrayaud, Sandrine and Floersheim, Philipp and Carcache, David and Urwyler, Stephan and Kallen, Joerg (2017) Design and synthesis of Selurampanel, a novel orally active and competitive AMPA receptor antagonist. ChemMedChem : chemistry enabling drug discovery, 12 (3). pp. 197-201. ISSN 18607179

Abstract

A series of potent quinazolinedione sulfonamide AMPA receptor antagonists were designed and synthesized. The SAR and in vivo activity of the series were investigated. In particular, compound 1S (Selurampanel) has shown excellent oral potency against MES-induced generalized tonic-clonic seizures in rodents. The X-ray structure of Selurampanel bound to AMPA was also obtained.

Item Type: Article
Date Deposited: 31 May 2017 00:45
Last Modified: 31 May 2017 00:45
URI: https://oak.novartis.com/id/eprint/29186

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