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

DOI: 10.1016/j.bmcl.2011.12.009

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 996 - 999 (2012)

Update date:2022-08-02

Topics:

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

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Article abstract of DOI:10.1016/j.bmcl.2011.12.009

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.

Full text of DOI:10.1016/j.bmcl.2011.12.009

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